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

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 pote...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 15; no. 7; pp. 1841 - 1845
Main Authors Kravchenko, Dmitri V, Kysil, Vladimir V, Ilyn, Alexey P, Tkachenko, Sergey E, Maliarchouk, Sergey, Okun, Ilya M, Ivachtchenko, Alexandre V
Format Journal Article
LanguageEnglish
Published England 01.04.2005
Subjects
Caspase 3
Caspase Inhibitors
Caspases - metabolism
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacology
Humans
Inhibitory Concentration 50
Quinolines - chemical synthesis
Quinolines - pharmacology
Structure-Activity Relationship
Online AccessGet full text

Cover

More Information
Summary: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 IC(50)=4 nM.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.02.027