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J Med Chem. 2011 Oct 13;54(19):6734-50. doi: 10.1021/jm200629m. Epub 2011 Sep 7.

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.

Author information

1
Cancer & Infection Research Area, AstraZeneca, Alderley Park, Macclesfield, Cheshire, SK10 4TG, United Kingdom. Maria-Elena.Theoclitou@astrazeneca.com

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 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.

PMID:
21899292
DOI:
10.1021/jm200629m
[Indexed for MEDLINE]
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