2. Academic Validation
  3. Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay

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

  • Bioorg Med Chem Lett. 2011 Apr 15;21(8):2192-7. doi: 10.1016/j.bmcl.2011.03.015.
Wenhua Chu 1,  Justin Rothfuss,  Dong Zhou,  Robert H Mach
Affiliations

Affiliation

  • 1 Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
PMID: 21441025 DOI: 10.1016/j.bmcl.2011.03.015
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.

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