Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: Introduction of a hydrophilic group increases potency in a whole cell assay

Wenhua Chu, Justin Rothfuss, Dong Zhou, Robert H. MacH

Research output: Contribution to journalArticlepeer-review

40 Scopus citations

Abstract

A series of isatin analogs containing a hydrophilic group, including a pyridine ring, ethylene glycol group, and a triazole ring, have been synthesized, and their inhibition potency for caspase-3 was measured both in vitro (i.e., recombinant enzyme) and in whole cells (HeLa cells). The analogs having a hydrophilic group, including 12, 13, 16, 38, and 40, have dramatically increased activity in vitro and in HeLa cells compared to the corresponding unsubstituted N-phenyl isatin analogs.

Original languageEnglish
Pages (from-to)2192-2197
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number8
DOIs
StatePublished - Apr 15 2011

Keywords

  • Apoptosis
  • Caspase-3
  • Cell death

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