Synthesis and Structure−Activity Relationship of 4-Substituted 2-(2-Acetyloxyethyl)-8-(morpholine- 4-sulfonyl)pyrrolo[3,4-c]quinoline- 1,3-diones as Potent Caspase-3 …
DV Kravchenko, YA Kuzovkova, VM Kysil… - Journal of medicinal …, 2005 - ACS Publications
DV Kravchenko, YA Kuzovkova, VM Kysil, SE Tkachenko, S Maliarchouk, IM Okun…
Journal of medicinal chemistry, 2005•ACS PublicationsSynthesis, biological evaluation, and SAR dependencies for a series of novel 1, 3-dioxo-2, 3-
dihydro-1 H-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.
dihydro-1 H-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.
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.
ACS Publications