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…

Index: 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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Citation Number: 22

Abstract

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 ...