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

journal contribution
posted on 2023-06-08, 05:29 authored by Kwai-Ming J Cheung, Thomas P Matthews, Karen James, Martin G Rowlands, Katherine J Boxall, Swee Y Sharp, Alison Maloney, S Mark Roe, Chrisostomos ProdromouChrisostomos Prodromou, Laurence PearlLaurence Pearl, G Wynne Aherne, Edward McDonald, Paul Workman
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.

History

Publication status

  • Published

Journal

Bioorganic and Medicinal Chemistry Letters

ISSN

0960-894X

Publisher

Elsevier

Issue

14

Volume

15

Page range

3338-3343

Department affiliated with

  • Biochemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2012-02-06

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