Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 13, Pages 4212-4215Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm050355z
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The crystal structure of a previously reported screening hit 1 (CCT018159) bound to the N terminal domain of molecular chaperone Hsp90 has been used to design 5-amide analogues. These exhibit enhanced potency against the target in binding and functional assays with accompanying appropriate cellular pharmaeodynamic changes. Compound 11 (VER-49009) compares favorably with the clinically evaluated 17-AAG.
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