758721-92-5Relevant academic research and scientific papers
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 spindle protein inhibitor and potential anticancer agent
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
, p. 6734 - 6750 (2011/12/04)
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 the monopolar spindle phenotype characteristic of KSP inhibition and induction of cellular death. A favorable pharmacokinetic profile and notable in vivo efficacy supported the selection of this compound as a clinical candidate for the treatment of cancer.
Bicyclicpyrimidones and their use to treat diseases
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, (2008/06/13)
The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest.
