2005

Pyrazole derivativesR 0180 The Identification, Synthesis, Protein Crystal Structure and in vitro Biochemical

Evaluation of a New 3,4-Diarylpyrazole Class of Hsp90 Inhibitors. — High-throughput screening of a library of 50,000 compounds identified 3,4-diarylpyra-zole CCT018159 (I) as a novel and potent inhibitor of Hsp90 ATPase. The synthesis of (I) and a number of close analogues is described and some structure—activity relation-ships are discussed. — (MCDONALD*, E.; et al.; Bioorg. Med. Chem. Lett. 15 (2005) 14, 3338-3343; Cancer Res. UK Cent. Cancer Therap., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK; Eng.) — C. Hettrich

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