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Letters in Drug Design & Discovery

Author(s): Dmitri V. Kravchenko, Julia A. Kuzovkova, Volodymyr M. Kysil, Sergey E. Tkachenko, Sergey Malarchuk, Ilya M. Okun and Alexandre V. Ivachtchenko

DOI: 10.2174/157018006775240908

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Pyrrolo[3,4-c]Quinoline-1,3-Diones as Potent Caspase-3 Inhibitors: Synthesis and SAR of 8-Sulfamoyl-1,3-Dioxo-2,3-Dihydro-1H-Pyrrolo[3,4- c]Quinolines

Page: [61 - 70] Pages: 10

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Abstract

Synthesis, biological evaluation and structure-activity relationships for a series of 8-sulfamoyl-1,3- dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines are described. These compounds represent a new chemotype of nonpeptide small molecule inhibitors of caspase-3. Among the studied compounds, several potent inhibitors have been identified. The most active compounds within this series inhibited caspase-3 with IC50 in the range of 23-30 nM.

Keywords: Caspase-3, inhibitor, 8-sulfamoyl-1,3-dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines, heterocycles, parallel synthesis, compound libraries