Title of article
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors
Author/Authors
Kwai-Ming J. Cheung، نويسنده , , Thomas P. Matthews، نويسنده , , Karen James، نويسنده , , Martin G. Rowlands، نويسنده , , Katherine J. Boxall، نويسنده , , Swee Y. Sharp، نويسنده , , Alison Maloney، نويسنده , , S. Mark Roe، نويسنده , , Chrisostomos Prodromou، نويسنده , , Laurence H. Pearl، نويسنده , , G. Wynne Aherne، نويسنده , , B. Edward McDonald and William L. Siegmann، نويسنده , , Paul Workman، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
3338
To page
3343
Abstract
High-throughput screening identified the 3,4-diarylpyrazole CCT018159 as a novel and potent (7.1 μM) 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.
Keywords
Hsp90 inhibitors , cancer , Protein crystal structure , resorcinol , Pyrazole
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795785
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