Bioorganic and Medicinal Chemistry Letters p. 1841 - 1845 (2005)
Update date:2022-09-26
Topics:
Kravchenko, Dmitri V.
Kysil, Vladimir V.
Ilyn, Alexey P.
Tkachenko, Sergey E.
Maliarchouk, Sergey
Okun, Ilya M.
Ivachtchenko, Alexandre V.
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 = 4 nM.
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