Targeting the heat shock protein 90 dimer with dimeric inhibitors.
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ABSTRACT:
SUBMITTER: Kusuma BR
PROVIDER: S-EPMC3184553 | biostudies-literature | 2011 Sep
REPOSITORIES: biostudies-literature
Publications
Targeting the heat shock protein 90 dimer with dimeric inhibitors.
Kusuma Bhaskar Reddy BR Peterson Laura B LB Zhao Huiping H Vielhauer George G Holzbeierlein Jeffrey J Blagg Brian S J BS
Journal of medicinal chemistry 20110823 18
The design, synthesis, and biological evaluation of conformationally constrained coumermycin A1 analogues are reported. Compounds were evaluated against both breast cancer (SKBr3 and MCF7) and prostate cancer (PC3 mm2, A549, and HT29) cell lines. Non-noviosylated coumermycin A1 analogues that manifest potent antiproliferative activity resulting from Hsp90 inhibition are provided, wherein replacement of the stereochemically complex noviose sugar with readily available piperidine rings resulted in ...[more]
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