1,3-dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors

被引：62

作者：

Kravchenko, DV

Kysil, VV

Ilyn, AP

Tkachenko, SE

Maliarchouk, S

Okun, IM

Ivachtchenko, AV ^{[1
]}

机构：

[1] ChemDiv Inc, San Diego, CA 92121 USA

[2] Chem Divers Res Inst, Dept Organ Chem, Chimki 114401, Moscow Region, Russia

[3] Chem Divers Res Inst, Dept Med Chem, Chimki 114401, Moscow Region, Russia

[4] Chem Divers Res Inst, Dept Mol Biol & High Temp Screening, Chimki 114401, Moscow Region, Russia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 07期

关键词：

caspase-3; inhibitor; 1H-pyrrolo[3,4-c]quinoline;

D O I：

10.1016/j.bmcl.2005.02.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-pyr-rolo [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. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1841 / 1845

页数：5

共 17 条

[1]

ANSELMO D, 2002, AM J TRANSPLANT, V2, P920

[2] SOME N-SUBSTITUTED 2-AMINO QUINOLINE-3,4-DICARBOXIMIDES-AND 2-METHYLQUINOLINE-3,4-DICARBOXIMIDES [J].