Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9769171 | European Journal of Medicinal Chemistry | 2005 | 7 Pages |
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 3-10Â nM have been identified. The most active compound within this series, 7{49} and 7{58}, inhibited caspase-3 with IC50Â =Â 3Â nM.
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Authors
Dmitri V. Kravchenko, Volodymyr M. Kysil, Sergey E. Tkachenko, Sergey Maliarchouk, Ilya M. Okun, Alexandre V. Ivachtchenko,