Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 11, Pages 3680-3683Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm048987t
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Synthesis, biological evaluation, and SAR dependencies for a series of novel 1,3-dioxo-2,3-dihydro-1H-pyrrolo-[3,4-c]quinoline inhibitors of caspase-3 are described. The inhibitory activity of the synthesized compounds is highly dependent on the nature of 4-substituents on the core scaffold. 4-Methyl-and 4-phenyl-substituted derivatives, which were the most active compounds within this series, inhibited caspase-3 with IC50 of 23 and 27 nM, respectively.
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