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Bioorg Med Chem Lett. 2011 Apr 15;21(8):2278-82. doi: 10.1016/j.bmcl.2011.02.101. Epub 2011 Feb 28.

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

Author information

1
Medicinal Chemistry, Pfizer, 401 N. Middletown Road, Pearl River, NY 10965, USA. christoph.zapf@pfizer.com

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.

PMID:
21420297
DOI:
10.1016/j.bmcl.2011.02.101
[Indexed for MEDLINE]

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