1, 3-Dioxo-4-methyl-2, 3-dihydro-1H-pyrrolo [3, 4-c] quinolines as potent caspase-3 inhibitors

…, VV Kysil, AP Ilyn, SE Tkachenko, S Maliarchouk…

Index: Kravchenko, Dmitri V.; Kysil, Vladimir V.; Ilyn, Alexey P.; Tkachenko, Sergey E.; Maliarchouk, Sergey; Okun, Ilya M.; Ivachtchenko, Alexandre V. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 7 p. 1841 - 1845

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Citation Number: 48

Abstract

Synthesis, biological evaluation and structure–activity relationships for a series of novel nonpeptide small molecule inhibitors of caspase-3 are described. Among the studied compounds, 8-sulfamide derivatives of 1, 3-dioxo-4-methyl-2, 3-dihydro-1H-pyrrolo [3, 4-c] quinolines have been identified as potent inhibitors of caspases-3. The most active compound within this series (8f) inhibited caspase-3 with IC50= 4nM.