Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation...

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Prof. Gary Gellerman Personal: Full Name:Gary Gellerman Date of birth:27/9/1962 Place of birth:USSR Date of immigration: October 25, 1978 Regular military service: 1984-1987. Home Address: 45 Ha’Yahalom Street Neve Yam,Rishon Le Zion, 74536 Telephon: 03-9510178, 054 7567067 E-mail: [email protected] Marital Status: Married + 2 children Citizenship: Israel. Languages: Hebrew, English, Russian Education B.Sc., 1985 - 1987: Ben Gurion University, Dep. of Chemistry, Track: Biophysical Chemistry, Beer Sheva, Israel. M.Sc. (Excellence), 1988- 1990: Tel Aviv Un., Ramat Aviv, Israel, Dep. of Chemistry, “Synthesis towards marine alkaloids” Research supervisor: Prof. Y. Kashman. Ph.D. 1990 - 1994: , Tel Aviv Un., Dep. of Chemistry, Ramat Aviv, Israel, “Synthesis of 7H-Pyrido[2,3,4-k]acridine alkaloids”Research supervisor: Prof. Y. Kashman. MBA 1990 - 1995: Tel Aviv Un., Dep. of Management, Ramat Aviv, Israel, Track: Technology and System Operation Management. Employment History 2013 present: Associate Professor, , Dept. Biological Chemistry, Faculty of Exact Sciences, Ariel University 2005-2013 Senior Lecturer, Dept. Biological Chemistry, Faculty of Exact Sciences, Ariel University Center of Samaria, Israel 2001-2004 VP Molecular Diversity, Chemistry Division, Compugen Ltd, Israel 1994-2001 Head of research group and project manager, Peptor Ltd, Israel Professional Activities: 2013 Present: Head of Dep. of Biological Chemistry, Faculty of Exact Sciences, Ariel University, Israel. Membership in Professional Societies Chairman of ISCT -2001-present: ISCT The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. Member, ICS Israeli Chemical Society Scientific experience Medicinal, organic, heterocyclic, peptide, peptidomimetic and combinatorial chemistries; Drug Design; Fluorescent Linkers; Targeted Drug Delivery; Explosive detection.

Transcript of Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation...

Page 1: Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. ... From Innovation and Perspectives

Prof. Gary Gellerman

Personal: Full Name:Gary Gellerman

Date of birth:27/9/1962

Place of birth:USSR

Date of immigration: October 25, 1978

Regular military service: 1984-1987.

Home Address: 45 Ha’Yahalom Street Neve Yam,Rishon Le Zion, 74536

Telephon: 03-9510178, 054 7567067

E-mail: [email protected]

Marital Status: Married + 2 children

Citizenship: Israel.

Languages: Hebrew, English, Russian

Education

B.Sc., 1985 - 1987: Ben Gurion University, Dep. of Chemistry, Track:

Biophysical Chemistry, Beer Sheva, Israel.

M.Sc. (Excellence), 1988- 1990: Tel Aviv Un., Ramat Aviv, Israel, Dep. of

Chemistry, “Synthesis towards marine alkaloids” Research

supervisor: Prof. Y. Kashman.

Ph.D. 1990 - 1994: , Tel Aviv Un., Dep. of Chemistry, Ramat Aviv,

Israel, “Synthesis of 7H-Pyrido[2,3,4-k]acridine

alkaloids”Research supervisor: Prof. Y. Kashman.

MBA 1990 - 1995: Tel Aviv Un., Dep. of Management, Ramat Aviv,

Israel, Track: Technology and System Operation Management.

Employment History 2013 – present: Associate Professor, , Dept. Biological Chemistry, Faculty of Exact

Sciences, Ariel University

2005-2013 Senior Lecturer, Dept. Biological Chemistry, Faculty of Exact

Sciences, Ariel University Center of Samaria, Israel

2001-2004 VP Molecular Diversity, Chemistry Division, Compugen Ltd, Israel

1994-2001 Head of research group and project manager, Peptor Ltd, Israel

Professional Activities:

2013 – Present: Head of Dep. of Biological Chemistry, Faculty of Exact Sciences,

Ariel University, Israel.

Membership in Professional Societies

Chairman of ISCT -2001-present:

ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS-

European Society of Combinatorial Sciences.

Member, ICS – Israeli Chemical Society

Scientific experience

Medicinal, organic, heterocyclic, peptide, peptidomimetic and combinatorial

chemistries; Drug Design; Fluorescent Linkers; Targeted Drug Delivery; Explosive

detection.

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Scientific Publications

1. “Synthesis of Pyrido[2,3.4-kl]Acridines. A Building Block for synthesis

of pyridoacridine alkaloids”, Gellerman G., Rudi A., Kashman Y.,

Tetrahedron Letters, 33, 5577-5580, 1992.

2. “Biomimetic Synthesis of Pyrido[2,3.4-kl]Acridines”, Gellerman G.,

Rudi A., Kashman Y., Tetrahedron Letters, 34, 1823-1826, 1993.

3. “A Two Step Biomimetic Total Synthesis of Eilatin”, Gellerman G.,

Babad M., Kashman Y., Tetrahedron Letters, 34, 1827-1830, 1993.

4. “Biomimetic Synthesis of Ascididemin and Derivatives”, Gellerman G.,

Rudi A., Kashman Y., Synthesis, 3, 239-241, 1994.

5. “The Biomimetic Synthesis of Marine Alkaloide releated Pyrido- and

Pyrrolo[2,3.4-kl]Acridines”, Gellerman G., Rudi A., Kashman Y.,

Tetrahedron, 50, 12959-12972, 1994.

6. “Potent Antileukemic Effect of some Pyridoacredine Alkaloides”, Einat

M., Elishner M., Nagler A., Fabian I., Gellerman G., Rudi A., Kashman

Y., Clinical Censer Research, 1, 823-829, 1995.

7. ”A Backbone-Cyclic, receptor 5 selective somatostatin analogue:

synthesis, bioactivity, and NMR conformational analysis” Gilon C.,

Huenges M., Matha B., Gellerman G., Kessler H., Journal of Medicinal

Chemistry, 41, 919-929, 1998.

8. “Facil Synthesis of Orthogonally Protected Amino Acid Building Blocks

for Combinatorial and Backbone Cyclic Peptide Chemistry”, Gellerman

G., Elgavi A., Kramer M., Journal of Peptide Research, 57, 277-290,

2001.

9. “Human Somatostatin Receptor Specificity of Backbone-Cyclic

Analogues Containing Novel Sulfur Building Units”, Gazal S.,

Gellerman G., Ziv O., Karpov O., Litman P., Bracha M., Afargan M.,

Gilon C., Journal of Medicinal Chemistry, 45, 1665-1671, 2002.

10. ”Synthesis of Novel Protected N(-thioalkyl) Amino Acid Building

Units and their Incorporation in Backbone Cyclic Disulfide and

Thioetheric Bridged Peptides” Gazal S., Gellerman G., Glukhov E.,

Gilon C., Journal of Peptide Research, 58, 527-539. 2001.

11. “Bioactive Somatostatin Analog Without a type II' beta-turn: Synthesis

and Conformational Analysis in Solution”. Jiang S., Gazal S., Gellerman

G., Ziv O., Karpov O., Litman P., Bracha M., Afargan M., Gilon C.,

Goodman M. A., Journal of Peptide Science, 7, 521-528, 2001.

12. “Novel Gly Building Units for Backbone Cyclization: Synthesis and

Incorporation Into Model Peptides”. Gazal S, Gellerman G, Gilon C.,

Peptides, 24, 1847-1852, 2003.

13. “Long-Acting SST Analog with Endocrine Selectivity: Potent

suppression of Growth Hormone but not of Insulin”. Afargan M., Tiensuu

E., Gellerman G., Oberg K., Endocrinology, 142, 477-486, 2001.

14. “Toward a PKB Inhibitor: Modification of a Selective PKA Inhibitor by

Rational Design”, Reuveni H., Livnah N., Geiger T., Klein S., Ohne O.,

Cohen I., Benhar M., Gellerman G., Levitzki A., Biochemistry, 41,

10304-10314, 2002.

15. “A facile two-step synthesis of Novel ring-A double substituted

tryptophan building blocks for combinatorial chemistry”, Gorohovsky S.,

Meir S., Shkoulev V., Byk G., Gellerman G., Synlett, 10, 1411-1414,

2003.

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16. “Dilactams. Synthesis of nonsymmetrical dibenzodiazocinediones”, Hassner

A., Sun B., Gellerman G., Meir S., Tetrahedron Letters, 45, 1377-1379, 2004.

17. “New application of DPPA reagent: one pot transformation of quinolin-

4-one and pyridin-4-one derivatives into 4-azido and 4-amino

counterparts.” Aizikovich A., Kuznetsov V., Gorohovsky S., Levy A.,

Meir S., Byk G., Gellerman G., Tetrahedron Letters, 45, 4241-4243,

2004.

18. “Approaches for introducing high molecular diversity in scaffolds: Fast Parallel

Synthesis of Highly Substituted 1H-quinolin-4-one Libraries” Kuznetsov V.,

Gorohovsky S., Levy A., Meir S., Shkoulev V., Menashe N., Greenwald M.,

Aizikovich A., Ofer D., Byk G., Gellerman G., Molecular Diversity, 8, 437-448,

2004.

19. "Reductive Nitrosation of Peptides Ligated to High Valent Metal

Cations", Shamir D., Zilbermann I., Maimon E., Gellerman G., Cohen

H., Meyerstein D., Eur. Jour. Inorg. Chem., 32, 5029-5031, 2007.

20. "Facile Synthesis of Orthogonally Protected Optically Pure Keto- and

Diketopiperazine Building Blocks for Combinatorial Chemistry”, Gellerman

G., Hazan E., Albeck A., Shatzmiler S., Intern. Jour. Pep. Res. Ther, 14, 183-

192, 2008.

21. "Synthesis of Orthogonally Protected Optically Pure Ketopiperazine,

Diketopiperazine, Ketodiazepane and 3-Aminopyrrolidone Building Blocks

for Peptidomimetic Combinatorial Chemistry", Gellerman G., Hazan E.,

Albeck A., Shatzmiler S., Tetrahedron, 65, 1389–1396, 2009.

22. "Synthesis of chiral heteronucleotide ONA sequences by a Fmoc/Boc-based

submonomeric strategy" Amir A., Hetsron A., Shatzmiller S., Gellerman G.,

Intern. Jour. Pep. Res. Ther., 15, 241-246, 2009.

23. "Synthesis and Antifungal Activity of β-Trifluroalkyl Aminovinyl Ketone

Derivatives", Gellerman G., Pariente N., Paz Z., Shneiderman A., Yarden O.,

Jour. Agric. Food Chem., 57, 8303-8307, 2009.

24. "Antibiotic- photosensitizer conjugates- a novel class of antibacterial

molecules", Cahan R., Swissa N., Gellerman G., Nitzan Y., Photochemistry

and Photobiology, 20, 675-683, 2009.

25. "One-pot derivatization of medicinally important 9-aminoacridine by

reductive amination and SNAr" Gellerman G.,Gaisin N.,Brider T.

Tetrahedron Lett., 51,836–839, 2010.

26. "Phenols - useful templates for the synthesis of bi-functional orthogonally

protected dendron building blocks via Solid Phase Mitsunobu reaction",

Gellerman G., Shitrit S., Shalit T., Ganot O., Albeck A., Tetrahedron, 66,

878–886, 2010.

27. "A double heteroatom Mitsunobu coupling with amino hydroxybenzoic acids

on solid phase: a novel aspect of Mitsunobu reaction to form dendron building

blocks." Shalit T., Albeck A., Gellerman G., Tetrahedron Lett., 51, 5988–

5991, 2010.

28. "One-Pot Synthesis of Novel Antiproliferative 9-Aminoacridines".

Gellerman G., Waintraub S., Gaisin V., Eur. Jour. Org. Chem., 22, 4176–

4182, 2011.

29. "A fast entry to the novel medicinally important 9-anilinoacridine peptidyls

by solid phase organic synthesis (SPOS)", Brider T., Gilad Y., Gellerman G.,

Tetrahedron Lett., 52, 3640-44, 2011.

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30. " Recent Synthetic Approaches to anticancer 9-anilinoacridines. A Review",

Gellerman G., Org. Prep. Proced. Inter., 44, 187–221, 2012.

31. "A two-step synthesis of medicinally-important 1,8-naphthalimide peptidyls

by solid phase organic synthesis (SPOS)" Brider T., Gellerman G.,

Tetrahedron Lett., 53, 5611–5615, 2012.

32. "Facile synthesis of potential antitumor novel N(9) methylated AHMA

analogs", Redko B., Albeck A., Gellerman G., New Jour. Chem., 36, 2188–

2191, 2012.

33. " Targeted drug delivery for cancer therapy: the other side of antibodies"

Firer M. A., Gellerman G., , Jour. Hematol. Oncol., 5:70, 1-16, 2012.

34. "MBP-chlorambucil conjugates: Improving the efficacy of targeted drug

delivery to murine models of Multiple Myeloma (MM) cells", Gellerman G.,

Baskin S., Yosef G., Firer M. A., Anti-Cancer Drugs, 24, 112-119, 2013.

35. "Penta-glycine-Ni(II) Complex: From Kinetics to Structure", Gaisin Z.,

Gellerman G., Meyerstein D., Eur. Jour. Inorg. Chem., 3191–3194, 2013.

36. "Switch off/switch on” regulation of drug cytotoxicity by conjugation to a cell

targeting peptide Gilad Y., Firer M. A., Rozovsky A., Ragozin E., Redko B.,

Albeck A., Gellerman G., Eur. Jour. Med. Chem., 85, 139-146, 2014

37. ''Three overlooked chemical approaches toward 3-naphtalimide amonafide N-

derivatives'' Brider T., Grynszpan F., Gellerman G., Tet. Lett., 55, 6675-

6679, 2014.

38. "Anti-proliferative activity of the combination of salan Ti(IV) complexes

with other organic and inorganic anticancer drugs against HT-29 and

NCIH1229 cells: synergism with cisplatin" Ganot N., Redko B., Gellerman

G., Tshuva E. Y., RSC Adv., 5, 7874–7879, 2015.

39. " Synthesis of novel antitumor carbazole-amonafide structural hybrids" Rozovsky A., Regozin E., Oron-Herman M., Albeck A., Gellerman G., Eur.

J. Org. Chem, 1811–1818, 2015.

40. "Antiproliferative Effects of Novel Aminoacridine-Based Compounds"

Munder A., Moskovitz Y., Redko B., Levy A. R., Ruthstein S., Gellerman

G., Gruzman A. Med. Chem., 11, 373-38, 2015.

41. ''1,4-Dihydropyridine Cationic Peptidomimetics with Antibacterial Activity''

Lapidot I., Albeck A., Gellerman G., Shatzmiller S., Grynszpan F. Int. J.

Pept. Res. Ther. 2015, DOI 10.1007/s10989-015-9460-1.

42. "Synthesis and in-vitro anticancer evaluation of 1,8-naphthalimide N(4) and

S(4)-derivatives combining DNA intercalation and alkylation capabilities", T.

Brider, B. Redko, M. Oron-Herman, A. Cohen-Matzlich, G. Gerlitz,

Gellerman G.,* F. Grynszpan,* Res. Chem. Inter., 2015, DOI:

10.1007/s11164-015-2115-1.

43. "-Aminoisobutyric acid leads a fluorescent syn-bimane LASER probe across

the blood-brain barrier", I. Lapidot, D. Baranes, A. Pinhasov, Gellerman G.,

A. Albeck, F. Grynszpan, S. Shatzmiller, Med. Chem., 2015, DOI:

10.2174/1573406411666150518105010.

44. "Synthesis, drug release and biological evaluation of new anticancer drug-

bioconjugates containing somatostatin backbone cyclic analog as a targeting

moiety" Redko, B., Ragozin, E., Bazylevich, A., Tuchinsky, H., Albeck, A.,

Shekhter Zahavi, T., Oron-Herman, M., Kostenich, G., Gellerman, G. Pep.

Science (Biopolymers), 2015, DOI: 10.1002/bip.22694.

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45. "Recent Developments in the Synthesis and Applications of Anticancer

Amonafide Derivatives. A Mini Review", Gellerman G. Lett. Drug Des.

Discov., 2015, DOI: 10.2174/1570180812666150529205049.

Proceedings:

1. Backbone-cyclic peptides in peptide drug discovery? Full Text By Arad O.,

Afargan M., Diskin Y., Feller E., Gamliel A., Gellerman G., Goldwasser I.,

Hadas E., Hornik V., From Book of Abstracts, 211th ACS National Meeting,

New Orleans, LA, March 24-28,1996.

2. In situ generation of Fmoc amino acid chlorides for extremely difficult

couplings to sterically hindered secondary amines in solid-phase peptide

synthesis Falb E., Yechezkel T., Salitra Y., Gellerman G., Muller D., Gilon

C., Edited by Fields, Gregg B., Tam, James P., Barany, G., From Peptides for

the New Millennium, Proceedings of the American Peptide Symposium, 16th,

Minneapolis, MN, United States, June 26-July 1, 55-57, 2000.

3. Gozal S., Gellerman G., Gilon C., “Synthesis of Novel Protected N(-

thioalkyl) Amino Acid Building Units and their Incorporation into Backbone

Cyclic Disulfide Bridged Peptides”. Proceedings of the Seventh International

Symposium SPS & Combichem Libraries, Southampton, UK. 189-191, 2001.

4. Synthesis of novel protected Nα-(ω-thioalkyl) amino acid building units and

their incorporation into backbone cyclic disulfide bridged peptides Full Text

By, Sharon G., Gellerman, G., Karpov, O., Litman, P., Bracha, M., Afargan,

M., Gilon, C., Edited by Epton R., From Innovation and Perspectives in Solid

Phase Synthesis & Combinatorial Libraries: Peptides, Proteins and Nucleic

Acids--Small Molecule Organic Chemistry Diversity, Collected Papers,

International Symposium, 7th, Southampton, United Kingdom, Sept. 18-22,

189-191, 2002.

5. "Multi-tethered and orthogonally protected piperazine, diazepine and

pyrrolidone building blocks for fast "around-the-scaffold" drug design",

Gellerman G., Hazan E., Kovaliov M., Albeck A., Shatzmiler S., 30eps,

Helsinki, Sep., 2008.

6. "A double heteroatom Mitsunobu coupling with amino hydroxybenzoicacids

on solid phase: a novel application of the Mitsunobu reaction to form dendron

building blocks", Shalit T., Albeck A. Gellerman G., 31epc, Copenhagen, Sep.

5-9, 224-225, 2010.

7. "SPOS route to Novel 9-Anilinoacridine Derivatives: Biological Evaluation",

Gellerman G., Brider T., Budovsky A. Aronov S., 31epc, Copenhagen, Sep.

5-9, 230-231, 2010.

8. "A New Synthetic Strategy for Novel Antibacterial Hybrid Drug-Like

Molecules", Lapidot I.,, Zats G., Albeck A., Gellerman G., Shatzmiller S.,

31epc, Copenhagen, Sep. 5-9, 236-237, 2010.

Books:

Book: "Targeted Drug Delivery in Cancer Therapeutics", Research Signpost,

Kerala, India, 2010. Book chapter: "Targeted Dendrimers in Cancer Drug

Delivery Systems", Gellerman G. Firer M. A.

Patents and Patent Applications

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1. "Tumor and other cell growth- and differentiation-related biological

applications of alkaloids derived from the tunicate Eudistoma specific, and

purification, characterization, and synthesis of compounds", Spector I.,

Shochet N., Kashman Y., Rudi A., Gellerman G., U.S. (1995), US 5432172 A

19950711.

2. "Preparation of Eudistoma alkaloids as neoplasm inhibitors", Spector I.,

Shochet N., Kashman Y., Rudi A., Gellerman G.,, PCT Int. Appl. (1994), WO

9403433 A1 19940217.

3. "Preparation of conformationally constrained backbone cyclized

somatostatin analogs", Hornik V., Afargan M., Gellerman G., (Peptor Ltd.,

Israel). U.S. Pat. Appl. Publ. (2002), 30 pp., Cont.-in-part of Appl. No.

PCT/IL99/00329.

4. "Selectivity of conformationally constrained backbone cyclized somatostatin

analogs with respect to insulin, GH, and glucagon secretion and somatostatin

receptor binding", Hornik V., Gellerman G., Afargan M., (Peptor Limited,

Israel). U.S. (2002), 21 pp., Cont.-in-part of U.S. 6,051,554.

5. "Conformationally constrained backbone cyclized somatostatin analogs",

Hornik VV., Gellerman G., Afargan M., (Peptor Limited, Israel). U.S.

(2000), 18 pp., Cont.-in-part of U.S. 5,748,643.

6. "Preparation of conformationally constrained backbone cyclized somatostatin

analogs", Hornik V., Afargan M., Gellerman G., (Peptor Ltd., Israel), PCT

Int. Appl. (1999), 82 pp WO 9965508.

7. "Preparation of conformationally constrained backbone cyclized somatostatin

analogs and combinatorial libraries", Hornik V., Seri-Levy A., Gellerman G.,

Gilon C., (Peptor Ltd.,).U.S.(1998), 35 pp., Cont.-in-part of U.S. Ser. No.

488,159. US 5770687.

8. "Conformationally constrained backbone cyclized somatostatin analogs",

Hornik V., Seri-Levy A., Gellerman G., Gilon C., (Peptor Ltd., Israel), PCT

Int. Appl. (1998), 97 pp. WO 9804583.

9. "Tumor and other cell growth- and differentiation-related biological

applications of alkaloids derived from the tunicate Eudistoma specific, and

purification, characterization, and synthesis of compounds", Spector I.,

Shochet N., Kashman Y., Rudi A., Gellerman G., (Research Foundation of

State University of New York, USA), U.S. (1995), 42 pp. Cont.-in-part of

U.S. 5,278,168. US 5432172.

10. "Preparation of Eudistoma alkaloids as neoplasm inhibitors", Spector I.,

Shochet N., Kashman Y., Rudi A., Gellerman G., (Research Foundation of

State University of New York, USA).PCT Int. Appl. (1994), 109 pp. WO

9403433.

11. "Dendrimeric Platform for Controlled Drug Release", Gellerman G., Firer

M.A., Application No: 178645 (2006), PCT IL2007/001225.

12. "Piperazine-based scaffolds for solid phase synthesis of combinatorial

libraries and method for their preparation", Gellerman G., Application No:

186004 (2007).

13. "Multifunctional platforms for targeted delivery of heavy metal

drugs

substances",Application No: 186008, Our Ref: 22590/mic/07,

Gellerman G., (2007).

14. "Antibacterial surfaces", Gellerman G., Cahan R., US provisional,

application: 61/129,951, (2008).

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15. "Antifungal compounds and compositions", Gellerman G., Yarden

O., US provisional application: 61/193,278, (2008).

16. "Heterocyclic scaffolds useful for preparation of combinatorial

libraries and methos of preparation thereof", Gellerman G., WO

2009/037642 A1.

17. "Dendrimeric Platform for Controlled Release of Drugs", Gellerman G., Firer

M. A., US 12/444118 , 2009.

18. "Dendrimeric Platform for Controlled Release of Drugs", Gellerman G., Firer

M. A., EP 07827199.6, (2009).

19. "Derivatives 9-aminoacridines and preparation thereof", Gellerman G.,

61/256,992, (2009).

20. "Antimicrobial Compounds and Compositions" Gellerman G., Yarden O.,

Aizikovich A., PCT/IB2009/055016, (2009).

21. "9-aminoacridine derivatives and their preparation and uses", Gelleman G.,

AUC-001 US PROV 2, No. 61/379,502 (2010).

22. Gary Gellerman,Firer Michael Title: Dendrimeric Platform for Controlled

Release of Dr

Priority Application: IL178645 filed on October 16, 2006 Status: abandoned

in February 2010

23. Gary Gellerman,Firer Michael PCT: PCT/IL2007/001225 filed October 11,

2007 Published: April 24, 2008 WO2008/047345 Status: EXPIRED

24. Gary Gellerman,Firer Michael National Phase:

US12/444,118 fiiling date October 11, 2007 Published: April 29, 2010

US2010-0105857 Status: pending 25. Gary Gellerman, Firer Michael EP7827199.6 filing date October 11, 2007

Published: April 24, 2008 EP2081601 Status: pending

Presentations at Scientific Meetings

1. “Biogenesis and Biomimetic Synthesis of Pyrido [2,3.4-kl]Acridine

Alkaloides”, Gellerman G., Rudi A., Kashman Y.,The 59th

Annual Meeting of

the Israel Chemical Society, 1994.

2. “Biogenesis and Biomimetic Synthesis of Pyrido [2,3.4-kl]Acridine

Alkaloides”, Gellerman G., Rudi A., Kashman Y., Gordon conference Feb.

1994, Ventura CA.

3. “A new Marine Alkaloides- Structure and Synthesis”, Gellerman G., Rudi A.,

Kashman Y.,Second Swedish- Israeli Symposium on New Trends in Organic

Chemistry, August 1994.

4. “Biomimetic Synthesis of Cytotoxic Pyrido [2,3.4-kl]Acridine Alkaloides”,

Gellerman G., Rudi A., Kashman Y., International Research Congress on

Natural Products; Halifax, Nova Scotia, Canada, July 31, 1994.

5. “Backbone-Cyclic Peptides in Peptide Drug Discovery”, Arad O., Gellerman

G., Gamliel A.,Salitra Y.,The 211th

ACS National Meeting,New

Orleans,LA,March 24-26,1996.

6. “Peptor’s Backbone Cyclization Approach for Synthesis of Somatostatin

Analogs”, Gellerman G., Gamliel A., Wanger M., Shohat D., Arad O., The 62th

Annual Meeting of the Israel Chemical Society, 1997.

7. Oral presentation: “Peptor’s Multiple Parallel Synthesis (MPS) Technology for

Throughput Synthesis of Backbone Cyclic Peptides”, Gellerman G., 8th

International Conference on Polymer Based Technology, 1998.

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8. “Peptor’s Multiple Parallel Synthesis (MPS) Technology for Throughput

Synthesis of Backbone Cyclic Peptides”, Gellerman G., Hadas E., The 63th

Annual Meeting of the Israel Chemical Society, 1998.

9. Co- chairman: “The 1st Israeli CombiTech Symposium: Advances and

Aplications in Drug Discovery”, Gellerman G., Weizman Ins., October 14-15,

2001.

10. Oral presentation: “Fast Parallel Synthesis of Highly Substituted 1H-

quinoline-4-on Libraries”, Gellerman G., The 69th

Meeting of the Israel

Chemical Society, 2004.

11. Organizing chairperson: “The 3rd Congress of The Israel Association for

Medicinal Chemistry and Drug Development”, Gellerman G., Weizman Ins.,

25,3,2004

12. ”Synthesis of modified coupling reagents based on Bop Cl for low level

racemization", Malka D., Gellerman G., Mastai Y., Shatzmiler S., The 72

Meeting of ICS, 2007.

13. ”Study of the Alkylation Reactions of Anions Derived from Oxime Ethers",

Vladimir G., Hoz S., Gellerman G., Shatzmiller S., A The 72 Meeting of ICS,

2007.

14. "Synthesis of new anti bacterial agents based on the natural peptide

Dermaseptin S4", Malka R., Malka D., Gellerman G., Mastai Y., Shatzmiller

S., The 72 Meeting of ICS, 2007.

15. "Coating of gold plates with new anti bacterial agents based on the

natural peptide Dermaseptin S4". Malka R., Malka D., Gellerman G.,

Mastai Y., Shatzmiller S., Eurocombi 4, Firenze, July 15-18, 2007.

16. Member of the Program Advisory Committee, Chairman of

CombiChem session. The 73rd Meeting of the Israel Chemical Society-

Technion, February 4-5, 2008,

17. "The Facile Synthesis of Orthogonally Protected Multi-Functional

Platforms for Rapid Loading of Bio-Agents by SPOC",Shitrit S.,Shalit

T.,Sofer A.,Albeck A., Gellerman G.,73rd Meeting of the Israel Chemical

Society- Jerusalem,February 4-5, 2008 ,

18. "Synthesis of the chiral PNA based on Ornithine/Lysine backbone",

Amir A., Hetsron A., Gellerman G., Mastai Y., Shatzmiller S.,The 73rd

Meeting of the Israel Chemical Society- Jerusalem, February 4-5, 2008.

19. "(E)-3-amino-1-phenylprop-2-en-1-ones as Novel Antifungal

Compounds: Synthesis, Optimization and Biological Activity", Pariente N.,

Paz Z., Yarden O., Nudelman A., Gellerman G.,The73rd Meeting of the

Israel Chemical Society- Jerusalem, February 4-5, 2008.

20. Facile Synthesis of Orthogonally Protected Tri-Functional Optically Pure

Keto – and Diketopiperazine Scaffolds for using in SPOC", Hazan E.,

Brider T., Troube T., Albeck A., Shatzmiller S., Gellerman G., The 73rd

Meeting of the Israel Chemical Society- Jerusalem, February 4-5, 2008.

21. "Kinetics of Oxime-Ethers Reactions", Gaisin V., Gellerman G., Hoz S.

Shatzmiller S., The 73rd Meeting of the Israel Chemical Society- Jerusalem,

February 4-5, 2008.

22. "Facile Synthesis of Orthogonally Protected Optically Pure Keto- and

Diketopiperazine Building Blocks for SPOC", Gellerman G., 30eps,

Helsinki, Sep. 2008.

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23. "Antibiotics-photosensitizer conjugates as efficient antibacterial entities",

Cohen R., Swissa N., Gellerman G., Nitzan Y., the 74th

meeting of ICS, 8-9

Feb 2009, Israel.

24. "Peptides-Ni(II)-complexdes: formation, red-ox reactions and stability",

Gaisin V., Gellerman G., Meyerstein D., the 74th meeting of ICS, 8-9 Feb

2009. Israel.

25. "Multifunctional diazacyclic building blocks for fast around-the-scaffold drug

design", Gellerman G., Hazan E., Kovaliov M., Albeck A., Shatzmiller

S., the 74th meeting of ICS, 8-9 Feb 2009, Israel.

26. Member of the scientific committee, Chairman of CombiChem

session."Solid phase Mitsunobu reaction as an efficient way for the synthesis

of low-order orthogonally protected iso-dendrones from phenolic templates",

Shitrit S., Shalit T., Gellerman G., the 74th meeting of ICS, 8-9 Feb 2009,

Israel.

27. "Myelin Basic Protein (MBP) peptide as a carrier for targeted delivery of

drugs to murine models of Multiple Myeloma (MM) cells", Gellerman G.

Firer M. A Intracellular Delivery of Therapeutics Molecules: From Bench to

Bedside, August 31st – September 2

nd 2009, Montpellier, France.

28. "One-Pot derivatization of medicinally important 9-AAs by reductive

amination and SNAr",Gaisin V., Waintrov S., Gellerman G., 75th

ICS

meeting, Jan 25-26, 2010.

29. "Regiospesific derivatization of hydroxy and amino benzoic acids by

SPOC",Shalit T.,Gellerman G.,Albeck A.,31EPS Symposium

Copenhagen,Denmark, 5-9 September 2010.

30. "SPOS route to Novel 9-Anilinoacridine Derivatives: Biological Evaluation",

Gellerman G., Gaisin V., Waintraub S., Budovsky A., Aronov S., 31EPS

Symposium Copenhagen, Denmark, 5-9 September 2010.

31. "Novel Peptidyl 9-Anilinoacridines and Their Biological Evaluation: from

Solution to SPOS", Brider T., Aronov S., Gellerman G., 31EPS Symposium

Copenhagen, Denmark, 5-9 September 2010.

32. "The Synthesis of antibacterial Dihydropyridine based peptide -Drug

Hybrids", Lapidot L., Shatzmiller S., Gellerman G., Albeck A., 31EPS

Symposium Copenhagen, Denmark, 5-9 September 2010.

33. Oral Presentation: "Novel Medicinally Important 9-Anilinoacridine

conjugates and Their Biological Evaluation: from Solution to High

Throughput Solid Phase Chemistry", Gellerman G.,International Drug

Discovery Science and Technology,October 23-26,2010, Beijing.

34. Oral Presentation: "Novel 9-anilinoacridine conjugates as non-DNA

damaging anticancer candidates: synthesis and biological evaluation",

Gellerman G., 9th congress of The Israel Association of Medicinal

Chemistry, March 8, 2011, Weizmann Ins.

35. "B-cell leukemic drug resistance to chlorambucil is overcome by its

conjugation to a targeting peptide" FirerM. A., Gellerman G., Baskin S.,

February 23-25, 2012, 3rd

Int. meeting of Hematological Malignancies in

Hong Kong.

36. "Novel 9-anilinoacridines have significant therapeutic effect: cytotoxicity and

mechanism of action". Bogdansky M., Becker T., Karakov K., Gellerman G.,

Aronov S., DDBT 2012, Amsterdam.

37. Oral Presentation: "Design and fast production of novel anticancer materials:

building an array for drug discovery", Gellerman G., The Seventh

Page 10: Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. ... From Innovation and Perspectives

International Conference Material Technologies and Modeling, Ariel

University Center of Samaria, Ariel, Israel, August 20 - 23, 2012.

38. "The Synthesis of fluorescent amino acids Based on a syn-Bimane Moiety and

Their Incorporation in Dipeptide Mimics" Lapidot I., Gellerman G., Albeck

A., Pinhasov A.,Shatzmiller S, ISMC 2012, Berlin 1-7 Sep 2012.

39. "One-Pot Synthesis and Anticancer Effect of Novel 9-Anilinoacridine

Derivatives", Gellerman G.,Gruzman A.,Redko B.,Gaisin V.,Olevson

A.,ISMC 2012,Berlin 1 -7 Sep 2012.

40. "SPOS Route to Novel Anticancer 9-Anilinoacridine Peptidyls", Brider T.,

Gilad Y., Gellerman G., ISMC 2012, Berlin 1-7 Sep 2012.

41. "Facile Synthesis of Potential Antitumor N(9)-methylated AHMA analogues"

Redko B.,Albeck A., Gellerman G., ISMC 2012, Berlin 1-7 Sep 2012.

42. "Combination Therapy - Anticancer Salan Ti(IV) Complexes with Known

Chemotherapeutic Drugs" Ganot N., Gellerman G., Tshuva E. Y., The 78

Meeting of the Israel Chemical Society. 12-13 February 2013.

43. "Penta-glycine-Ni(II) Complex: From Kinetics to Structure" , Gaisin Z.,

Gellerman G., Meyerstein D., The 78 Meeting of the Israel Chemical Society.

12-13 February 2013.

44. Invited Speaker: " Development of novel multifunctional anticancer

conjugates for targeted chemotherapy ", Gellerman G., International

Conference on Biological and Biomedical Science (WCBBS), September

23rd

-27th

, 2013, Dares Salaam, Tanzania.

45. Oral Presentation: "Switch off/switch on” regulation of drug cytotoxicity by

conjugation to a cell targeting peptide", Gellerman G., 3‐rd International

Conference of Organic Chemistry Organic Synthesis ‐ Driving Force of Life

Development” ICOC‐2014(, ) September 25‐28, 2014, Tbilisi, Georgia.

46. Oral Presentation: Gellerman G., "Development of novel multifunctional

peptide-drugs conjugates for targeted chemotherapy

ANTIBODY/TARGETED-DRUG CONJUGATES conference, April 13-15,

2015 Park Atlantic, Porto, Portugal.

Research grants and contracts:

1. "Novel Medicinally Important Intercalating Conjugates and Their

Biological Evaluation" NOFAR 2011, collaboration with Teva.

2. MEIMAD, Chief Scientist, "Remote system for detection of traces of

explosives, drugs, nerve gases and radioactive materials (RSDS),

collaboration with Maavarim BS, 2013-2014.

3. Maavarim BS, Kidron, Israel, 2012-1013.

4. Judea & Samaria R&D grant 2013.

5. Ariel Un. R&D grant 2014.

6. "Development of novel peptide drug conjugate for anti-cancer therapy"

ACACR 2014.

7. "Development of novel peptide drug conjugate for anti-cancer therapy"

ACACR 2015.

Research grants awarded as "Very Good" (TOV MEOD) or suitable for

granting but didn't granted:

1. 97/08 ISF - "Multifunctional platforms for controlled drug release: Improving

the efficacy of targeted drug delivery to murine models of Multiple Myeloma

Page 11: Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. ... From Innovation and Perspectives

(MM) cells:" - TOV MEOD, was granted by Ariel Un. Center for 10.000

shekels

2. 3_3935 Ministry of Health, Chief Scientist Office-"Preclinical assessments on

use of M-protein specific peptides for TDD and follow up MM treatment in

patients" – deserves granting.

3. 98/09 ISF - "Multifunctional platforms for controlled drug release: Improving

the efficacy of targeted drug delivery to murine models of Multiple Myeloma

(MM) cells:" - TOV MEOD

Ph.D candidates: 1. Vladimir Gaisin, (2008-) "Reductive Nitrosations of Peptide –Metal complexes" Co-

supervisor with Prof. D. Meyerstein, Ariel University,

Israel

2. Tamara Brider, (2009-) "Synthesis of multifunctional privilege scaffolds for fast

around-the-scaffold" optimization by SPOC","Co-supervisor

with Prof. D. Meirstein, Ariel Un. Center of Samaria, Israel

3. Tzachi Shalit (2009-)Co-supervisor with Prof. A. Albeck, Bar-Ilan University,

Israel.

4. Inbal Lapidot (2009-2014) " The synthesis and exploration of novel synthesized

antimicrobial agents on the basis of antibacterial ultra-short

peptides and organic heterocycles", Co-supervisor with Prof.

A. Albeck, Bar-Ilan University, Israel and Prof. Shimon

Shatzmiler from Ariel University, Israel

5. Tamar Traube, (2008-2012) "Computer assisted design of novel serine protease

inhibitors: A combinatorial approach, applying EITA for the

design of TS analog chemical warheads and traditional

structure-based design of peptidomimetic recognition

elements", Co-supervisor with Prof. A. Albeck, Bar-Ilan

University, Israel

6. Yosi Gilat (2011-) "Development of multi drug-peptides conjugates for TDD" Co-

supervisor with Prof. A. Albeck, Bar-Ilan University, Israel

and Dr. Michael Firer from Ariel University, Israel

7. Redko Boris (2012- ) "Synthesis of novel heteroatoc containing anticancer polycyclic

compounds" Co-supervisor with Prof. A. Albeck, Bar-Ilan

University, Israel

8. Elena Ragozin (2013- ) "Synthetic strategies towards novel multi containing

anticancer conjugates" Co-supervisor with Prof. M.

Zinigrad, Ariel University, Israel

9. Andrey Bazilevich (2013- ) "Synthesis of novel fluorescent linkers for in vivo

imaging by TDD " Co-supervisor with Prof. D. Meyerstein,

Ariel University, Israel

10. Alex Rozovsky (2015- ) " Synthesis of novel fluorescent linkers for biodistribution

of peptide conjugates in targeted drug delivery" Co-

supervisor with Prof. D. Meyerstein, Ariel University, Israel

Former MSc. Candidates:

1. Sagit Shitrit, (2006-2008), "Development of multifunctional platforms for time

controlled targeted drug delivery",Co-supervisor with Prof.

S.Margel, Bar-Ilan University, Israel

Page 12: Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. ... From Innovation and Perspectives

2. Natali Pariente, (2006-2008)," Development of Antifungal Compounds Based on

Novel Trifluroalkyl β- Aminovenyl ketone and Triazole

Motives for Medicinal and Agricultural Uses", Co-

supervisor with Prof. A. Nudelman, Bar-Ilan University,

Israel

3. Aviran Amir, (2006-2008),"Synthesis of chiral Peptide Nucleic Acid (PNA) based

on Ornithine backbone", Co-supervisor with Prof. Y.

Mastai, Bar-Ilan University, Israel and Prof. Shimon

Shatzmiler from Ariel University, Israel

4. Amit Herson, (2006-2008),Synthesis toward chiral Peptide Nucleic Acid (PNA)

based on Ornithine backbone" , Co-supervisor with Prof. Y.

Mastai, Bar-Ilan University, Israel and Prof. Shimon

Shatzmiler from Ariel University Center, Israel

5. Tamara Brider, (2006-2008),"Synthesis and biological activity evaluation of

antibacterial peptides and synthesis of chiral 2,5-

diketopiperazes", Co-supervisor with Prof. A. Albeck, Bar-

Ilan University, Israel

6. Tamar Traube, (2006-2008)"Short peptides on ketopiperazine scaffolds as

antibacterial activities" Co-supervisor with Prof. A. Albeck,

Bar-Ilan University, Israel and Prof. Shimon Shatzmiler

from Ariel University, Israel

7. Eran Hazan (2006-2008)"Synthesis of chiral orthogonally protected milti-functional

ketopiperazine scaffolds for using in SPOC", Co-supervisor

with Prof. A. Albeck, Bar-Ilan University, Israel and Prof.

Shimon Shatzmiler from Ariel University, Israel

8. Tzachi Shalit (2007-2009)"Development of Pt-Drug platforms for targeted drug

delivery", Co-supervisor with Prof. A. Albeck, Bar-Ilan

University, Israel

9. Yosi Gilat (2009- 2011 )"Synthesis of loaded platforms with drugs for TDD" Co-

supervisor with Prof. A. Albeck, Bar-Ilan University,

Israel

10. Sagiv Waintrov (2009-2011) "One-pot derivatization of potent 9-aminoacridine"

Co- supervisor with Prof. A. Albeck, Bar-Ilan University,

Israel

11. Sofi Baskin,(2008- 2012)" Development of anticancer drug-peptide conjugates for

targeted drug delivery", Co-supervisor with Prof. A. Albeck,

Bar-Ilan University, Israel and Dr. Michael Firer from Ariel

University, Israel

12. Redko Boris(2010- 2012)"Development a linkage technology for anticancer

drugs" Co- supervisor with Prof. A. Albeck, Bar-Ilan

University, Israel.

13. Alex Rozovsky (2013-2015 ) " Synthesis of anticancer structural hybrids of

amonafide - carbazoles" Co-supervisor with Prof. A.

Albeck, Bar-Ilan University, Israel.

Department Promoting and Contributing Activities

Page 13: Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. ... From Innovation and Perspectives

a. Articles: Chemistry in Israel, Issue No. 23, January 2008: Education in Israel:

The Department of Biological Chemistry at the Academic College of

Judea and Samaria, by Gellerman G.

b. Evaluation of grants and scientific papers:

GIF 2008,

GIF 2009

GIF 2011

2 manuscripts from Int. J. Pept. Res. Ther, 2008.

Manuscript from peptide and protein letters, 2009.

Manuscript from Letters in Drug Design & Discovery, 2011.

Manuscript from ACS Combinatorial Science , 2012.

Manuscript from ACS Chemical Neuroscience 2013.

Manuscript from Bentham - Medicinal Chemistry 2013

Manuscript from Bentham – Letters in Drug Design & Discovery 2015

Manuscript from PLOS ONE 2015

Manuscript from Elsevier – Research on Chemical Intermediates 2015

Manuscript from MDPI – Pharmaceuticals 2015

Manuscript from Dove Medical Press –International Journal of Nanomedicine

(IF = 4.195), 2015

Manuscript from Current Topics in Medicinal Chemistry (IF = 3.453), 2015

Manuscript from European journal of Medicinal Chemistry (IF = 3.447), 2015

c. Invited speaker

6.3.2008, Ministry of Justice, Patent Authorities in Jerusalem. The title was:

"Development of multifunctional platforms for controlled TDD"

13.6.2012, Seminar in Dep. of Chemistry in Bar-Ilan university." Old drugs

new opportunities: synthetic perspective toward antitumor Amonafide,

Elinafide, Amsacrine and AHMA analogs".

d. Ph.D. thesis referee.

Evaluation of Ph.D thesis of Liron Levi-Beladev: "Using peptides to study

protein interactions"Under supervision of Prof. Assaf Friedler from Hebrew

Un. of Jerusalem, 2011.

Evaluation of Ph.D thesis of David Rosenthal: "Development of novel drug

leads for the treatment of pain."Under supervision of Prof. Chaim Gilon from

Hebrew Un. of Jerusalem, 2012.

Evaluation of Ph.D thesis of Shirly Naveh: "Development of chemical tools for

studying protein-protein interactions". Under supervision of Prof. Chaim Gilon

from Hebrew Un. of Jerusalem, 2012.

Evaluation of of Ph.D thesis of Alaa Talhami: "Development of novel methods for the

synthesis of backbone peptides and their implementation in development of peptide

leads ". Under supervision of Prof. Chaim Gilon from Hebrew Un. of Jerusalem, 2013.

Evaluation of Ph.D thesis of Ella Meltzer-Mats: "Design, Synthesis and

Mechanism of Hypoglycemic Activity of Bi-functional Benzothiazole

Derivatives, 2014.

Page 14: Prof. Gary Gellerman · ISCT –The Israeli Society of Combinatorial Technologies, the affiliation of ESCS- European Society of Combinatorial Sciences. ... From Innovation and Perspectives

Evaluation of Ph.D thesis of Patael Sigalit: "Transition state analog inhibitors

for the intarmembrane Rhomboid Proteases", 2015

e. Committees:

Head of the Chemistry department searching committee.

Member of Ariel University conference granting committee.

Member of ethic and discipline commission for staff.

f. Organizer of scientific tours for Ariel under graduate students in biotech

companies at scientific park in Rechovot 2008 and 2009.

g. Organizer of the faculty seminar, 15th on March, 2007, in Ariel University

Center with Prof. Anna Maria Papini from University of Florence, Italy. The

title of the seminar was: "A Chemical Reverse Approach to Detect Biomarkeers

of Autoimmune Diseases"