Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1, 2] thiazolo [5, 4-d] pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin …

…, J Ezhuthachan, S Filla, E Freed, H Hu…

文献索引：Theoclitou, Maria-Elena; Aquila, Brian; Block, Michael H.; Brassil, Patrick J.; Castriotta, Lillian; Code, Erin; Collins, Michael P.; Davies, Audrey M.; Deegan, Tracy; Ezhuthachan, Jayachandran; Filla, Sandra; Freed, Ellen; Hu, Haiqing; Huszar, Dennis; Jayaraman, Muthusamy; Lawson, Deborah; Lewis, Paula M; Nadella, Murali V. P.; Oza, Vibha; Padmanilayam, Maniyan; Pontz, Timothy; Ronco, Lucienne; Russell, Daniel; Whitston, David; Zheng, Xiaolan Journal of Medicinal Chemistry, 2011 , vol. 54, # 19 p. 6734 - 6750

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被引用次数: 22

摘要

Structure–activity relationship analysis identified (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3- methyl-4-oxo-[1, 2] thiazolo [5, 4-d] pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The selected compound arrested cells in mitosis leading to the formation of ...