2. Academic Validation
  3. Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity

Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity

  • Bioorg Med Chem Lett. 2011 Apr 15;21(8):2278-82. doi: 10.1016/j.bmcl.2011.02.101.
Christoph W Zapf 1,  Jonathan D Bloom,  Jamie L McBean,  Russell G Dushin,  Thomas Nittoli,  Charles Ingalls,  Alan G Sutherland,  John P Sonye,  Clark N Eid,  Jennifer Golas,  Hao Liu,  Frank Boschelli,  Yongbo Hu,  Erik Vogan,  Jeremy I Levin
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Pfizer, 401 N. Middletown Road, Pearl River, NY 10965, USA. christoph.zapf@pfizer.com
PMID: 21420297 DOI: 10.1016/j.bmcl.2011.02.101
Abstract

A novel series of macrocyclic ortho-aminobenzamide HSP90 inhibitors is reported. A basic nitrogen within the tether linking the aniline nitrogen atom to a tetrahydroindolone moiety allowed access to compounds with good physical properties. Important structure-activity relationship information was obtained from this series which led to the discovery of a soluble and stable compound which is potent in an HSP90 binding and cell-proliferation assay.

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