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ID: ALA1149510

Journal: Bioorg Med Chem Lett

Title: Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Authors: Kawanishi N, Sugimoto T, Shibata J, Nakamura K, Masutani K, Ikuta M, Hirai H.

Abstract: The design of a novel series of cyclin-dependent kinase (CDK) inhibitors containing a macrocyclic quinoxaline-2-one is reported. Structure-based drug design and optimization from the starting point of diarylurea 2, which we previously reported as a moderate CDK1,2,4,6 inhibitor [J. Biol.Chem.2001, 276, 27548], led to the discovery of potent CDK1,2,4,6 inhibitor that were suitable for iv administration for in vivo study.

CiteXplore: 16876403

DOI: 10.1016/j.bmcl.2006.07.026