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.
Original language | English |
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Pages (from-to) | 3338-3343 |
Journal | Bioorganic & Medicinal Chemistry Letters |
Volume | 15 |
Issue number | 14 |
DOIs | |
Publication status | Published - 15 Jul 2005 |