ChemInform Abstract: N-Propargyl-2-alkynylbenzothiazolium Aza-enediynes: Role of the...

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2002 benzothiazole derivatives benzothiazole derivatives R 0270 09 - 134 N-Propargyl-2-alkynylbenzothiazolium Aza-enediynes: Role of the 2-Alkynylbenzothiazolium Functionality in DNA Cleavage. Four compounds of type (V) and compound (VII) are prepared and tested as DNA cleavage agents. While compounds (V) are shown to be modest DNA agents, DNA cleavage is also observed with (VII). The structural requirements for DNA cleavage and the correlation of DNA cleavage efficiency with the propensity of these compounds to undergo nucleophilic addition by methanol support a proposed DNA cleavage mechanism involving DNA alkylation by appropriate 2-alkynyl-substituted benzothiazolium salts. — (KUMAR, DALIP; DAVID, WENDI M.; KERWIN, SEAN M.; Bioorg. Med. Chem. Lett. 11 (2001) 22, 2971-2974; Med. Chem. Div., Coll. Pharm., Univ. Tex., Austin, TX 78712, USA; EN) 1

Transcript of ChemInform Abstract: N-Propargyl-2-alkynylbenzothiazolium Aza-enediynes: Role of the...

2002 benzothiazole derivatives

benzothiazole derivativesR 0270

09 - 134N-Propargyl-2-alkynylbenzothiazolium Aza-enediynes: Role of the2-Alkynylbenzothiazolium Functionality in DNA Cleavage. — Fourcompounds of type (V) and compound (VII) are prepared and tested as DNAcleavage agents. While compounds (V) are shown to be modest DNA agents,DNA cleavage is also observed with (VII). The structural requirements for DNAcleavage and the correlation of DNA cleavage efficiency with the propensityof these compounds to undergo nucleophilic addition by methanol support aproposed DNA cleavage mechanism involving DNA alkylation by appropriate2-alkynyl-substituted benzothiazolium salts. — (KUMAR, DALIP; DAVID,WENDI M.; KERWIN, SEAN M.; Bioorg. Med. Chem. Lett. 11 (2001) 22,2971-2974; Med. Chem. Div., Coll. Pharm., Univ. Tex., Austin, TX 78712,USA; EN)

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