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
Dmitri V. Kravchenko,
Julia A. Kuzovkova,
Volodymyr M. Kysil,
Sergey E. Tkachenko,
Ilya M. Okun,
Alexandre V. Ivachtchenko.
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
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