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

Title: 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

Volume: 3 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Kravchenko V. Dmitri, Kuzovkova A. Julia, Kysil M. Volodymyr, Tkachenko E. Sergey, Malarchuk Sergey, Okun M. Ilya and Ivachtchenko V. Alexandre, 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, Letters in Drug Design & Discovery 2006; 3 (1) . https://dx.doi.org/10.2174/157018006775240908