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

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Chu W, Rothfuss J, Zhou D, Mach RH

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.

PubMed ID

21441025 [ View in PubMed

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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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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1-METHYL-5-(2-PHENOXYMETHYL-PYRROLIDINE-1-SULFONYL)-1H-INDOLE-2,3-DIONE	Caspase-3	EC 50 (nM)	7670	N/A	N/A	Details