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

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 and Workman, Paul (2005) The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. Bioorganic and Medicinal Chemistry Letters, 15 (14). pp. 3338-3343. ISSN 0960-894X

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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.

Item Type: Article
Schools and Departments: School of Life Sciences > Biochemistry
Depositing User: Mark Roe
Date Deposited: 06 Feb 2012 20:13
Last Modified: 05 Mar 2015 07:34
URI: http://srodev.sussex.ac.uk/id/eprint/24775
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