3, 4-Dihydropyrimido (1, 2-a) indol-10 (2H)-ones as potent non-peptidic inhibitors of caspase-3

…, V Marathias, G Tawa, A Aulabaugh, R Cowling…

Index: 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. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 22 p. 7755 - 7768

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Citation Number: 19

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 ( ...