Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors

…, S Ashwell, P Brassil, J Breed, J Ezhuthachan…

文献索引：Oza, Vibha; Ashwell, Susan; Brassil, Patrick; Breed, Jason; Ezhuthachan, Jaychandran; Deng, Chun; Grondine, Michael; Horn, Candice; Liu, Dongfang; Lyne, Paul; Newcombe, Nicholas; Pass, Martin; Read, Jon; Su, Mei; Toader, Dorin; Yu, Dingwei; Yu, Yan; Zabludoff, Sonya Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2330 - 2337

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被引用次数: 14

摘要

Checkpoint kinase 1 (Chk1, CHEK1) is a Ser/Thr protein kinase that plays a key role in mediating the cellular response to DNA-damage. Synthesis and evaluation of a previously described class of Chk1 inhibitors, triazoloquinolones/triazolones (TZs) is further described herein. Our investigation of structure–activity relationships led to the identification of potent inhibitors 14c, 14h and 16e. Key challenges included modulation of physicochemical ...