The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors |
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| Authors: | Cheung Kwai-Ming J Matthews Thomas P James Karen Rowlands Martin G Boxall Katherine J Sharp Swee Y Maloney Alison Roe S Mark Prodromou Chrisostomos Pearl Laurence H Aherne G Wynne McDonald Edward Workman Paul |
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| Affiliation: | 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. |
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| 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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