2. Academic Validation
  3. Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone

  • Bioorg Med Chem Lett. 2008 Dec 1;18(23):6273-8. doi: 10.1016/j.bmcl.2008.09.081.
Pei-Pei Kung 1,  Lee Funk,  Jerry Meng,  Michael Collins,  Joe Zhongxiang Zhou,  M Catherine Johnson,  Anne Ekker,  Jeff Wang,  Pramod Mehta,  Min-Jean Yin,  Caroline Rodgers,  Jay F Davies 2nd,  Eileen Bayman,  Tod Smeal,  Karen A Maegley,  Michael R Gehring
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, La Jolla Laboratories, 10770, Science Center Dr., San Diego, CA 92121, USA. peipei.kung@pfizer.com
PMID: 18929486 DOI: 10.1016/j.bmcl.2008.09.081
Abstract

Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a HSP90 competitive binding assay. A class of novel and potent small molecule HSP90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human Cancer cell lines in vitro, with IC(50) values averaging 20 nM.

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