Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists

Heidi L. Perez, Patrizia Banfi, Jay Bertrand, Zhen Wei Cai, James W. Grebinski, Kyoung Kim, Jonathan Lippy, Michele Modugno, Joseph Naglich, Robert J. Schmidt, Andrew Tebben, Paola Vianello, Donna D. Wei, Liping Zhang, Arturo Galvani, Louis J. Lombardo, Robert M. Borzilleri

Research output: Contribution to journalArticlepeer-review

Abstract

A series of phenylacylsulfonamides has been prepared as antagonists of Bcl-2/Bcl-xL. In addition to potent binding affinities for both Bcl-2 and Bcl-xL, these compounds were shown to induce classical markers of apoptosis in isolated mitochondria. Overall weak cellular potency was improved by the incorporation of polar functionality resulting in compounds with moderate antiproliferative activity.

Original languageEnglish
Pages (from-to)3946-3950
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number12
DOIs
Publication statusPublished - Jun 15 2012

Keywords

  • Apoptosis
  • Bcl-2
  • Bcl-xL
  • Isolated mitochondria
  • Protein-protein interaction

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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