Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 14, Pages 3338-3343Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.05.046
Keywords
Hsp90 inhibitors; cancer; pyrazole; resorcinol; protein crystal structure
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Funding
- Wellcome Trust Funding Source: Medline
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High-throughput screening identified the 3,4-diarylpyrazole CCT018159 as a novel and potent (7.1 mu M) 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. (c) 2005 Elsevier Ltd. All rights reserved.
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