1202497-85-5Relevant articles and documents
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3
Havran, Lisa M.,Chong, Dan C.,Childers, Wayne E.,Dollings, Paul J.,Dietrich, Arlene,Harrison, Boyd L.,Marathias, Vasilios,Tawa, Gregory,Aulabaugh, Ann,Cowling, Rebecca,Kapoor, Bhupesh,Xu, Weixin,Mosyak, Lidia,Moy, Franklin,Hum, Wah-Tung,Wood, Andrew,Robichaud, Albert J.
experimental part, p. 7755 - 7768 (2010/03/03)
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.