Design, synthesis, and biological evaluation of conformationally constrained cis-amide HSP90 inhibitors

Adam S. Duerfeldt, Gary E.L. Brandt, Brian S.J. Blagg

Research output: Contribution to journalArticlepeer-review

Abstract

Conformationally constrained cis-amide chimeric inhibitors of Hsp90 have been synthesized and evaluated for their Hsp90 inhibitory activity. These new compounds exhibited Hsp90 ATPase inhibition and induced Hsp90-dependent client protein degradation in a dose-dependent manner. Biological data reported herein suggests that amide bond isomerization of geldanamycin derivatives plays an important role in affinity for the heteroprotein complex present in cancer cells.

Original languageEnglish (US)
Pages (from-to)2353-2356
Number of pages4
JournalOrganic Letters
Volume11
Issue number11
DOIs
StatePublished - Jun 4 2009
Externally publishedYes

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