Format

Send to

Choose Destination
See comment in PubMed Commons below
Org Lett. 2009 Jun 4;11(11):2353-6. doi: 10.1021/ol900783m.

Design, synthesis, and biological evaluation of conformationally constrained cis-amide Hsp90 inhibitors.

Author information

1
Department of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, Kansas 66045-7562, USA.

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.

PMID:
19435295
PMCID:
PMC2697668
DOI:
10.1021/ol900783m
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for American Chemical Society Icon for PubMed Central
    Loading ...
    Support Center