Pyrrolo [3, 4-c] quinoline-1, 3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo [3, 4-c] quinoline-1 …

…, S Maliarchouk, IM Okun, AV Ivachtchenko

Index: Kravchenko, Dmitri V.; Kysil, Volodymyr M.; Tkachenko, Sergey E.; Maliarchouk, Sergey; Okun, Ilya M.; Ivachtchenko, Alexandre V. European Journal of Medicinal Chemistry, 2005 , vol. 40, # 12 p. 1377 - 1383

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Citation Number: 39

Abstract

Synthesis, biological evaluation and structure–activity relationships for a series of 2- substituted 4-methyl-8-(morpholine-4-sulfonyl)-1, 3-dioxo-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 with IC50 in the range of 3–10 nM have been identified. The most active ...