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  3. The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

  • Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43. doi: 10.1016/j.bmcl.2005.05.046.
Kwai-Ming J Cheung 1,  Thomas P Matthews,  Karen James,  Martin G Rowlands,  Katherine J Boxall,  Swee Y Sharp,  Alison Maloney,  S Mark Roe,  Chrisostomos Prodromou,  Laurence H Pearl,  G Wynne Aherne,  Edward McDonald,  Paul Workman
Affiliations

Affiliation

  • 1 Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK and Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK.
PMID: 15955698 DOI: 10.1016/j.bmcl.2005.05.046
Abstract

High-throughput screening identified the 3,4-diarylpyrazole CCT018159 as a novel and potent (7.1 microM) inhibitor of HSP90 ATPase activity. Here, we describe the synthesis of CCT018159 and a number of close analogues together with data on their biochemical properties. Some initial structure-activity relationships are discussed, as well as the crystal structure of CCT018159 bound to HSP90.

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