Title of article :
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3 Original Research Article
Author/Authors :
Lisa M. Havran، نويسنده , , Dan C. Chong، نويسنده , , Wayne E. Childers، نويسنده , , Paul J. Dollings، نويسنده , , Arlene Dietrich، نويسنده , , Boyd L. Harrison، نويسنده , , Vasilios Marathias، نويسنده , , Gregory Tawa، نويسنده , , Ann Aulabaugh، نويسنده , , Rebecca Cowling، نويسنده , , Bhupesh Kapoor، نويسنده , , Weixin Xu، نويسنده , , Lidia Mosyak، نويسنده , , Franklin Moy، نويسنده , , Wah-Tung Hum، نويسنده , , Andrew Wood، نويسنده , , Albert J. Robichaud، نويسنده ,
Abstract :
Cysteine-dependant aspartyl protease (caspase) activation has been implicated as a part of the signal transduction pathway leading to apoptosis. It has been postulated that caspase-3 inhibition could attenuate cell damage after an ischemic event and thereby providing for a novel neuroprotective treatment for stroke. As part of a program to develop a small molecule inhibitor of caspase-3, a novel series of 3,4-dihydropyrimido(1,2-a)indol-10(2H)-ones (pyrimidoindolones) was identified. The synthesis, biological evaluation and structure–activity relationships of the pyrimidoindolones are described.
Keywords :
apoptosis , Stroke , Pyrimidoindolone , Caspase-3
