| Literature DB >> 22632936 |
D Vijay Kumar1, Christophe Hoarau, Matthew Bursavich, Paul Slattum, David Gerrish, Kraig Yager, Michael Saunders, Mark Shenderovich, Bruce L Roth, Rena McKinnon, Ashley Chan, Daniel M Cimbora, Chad Bradford, Leslie Reeves, Scott Patton, Damon I Papac, Brandi L Williams, Robert O Carlson.
Abstract
Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter. Mps1 biochemical activity and cytotoxicity in HCT-116 cell line were improved. On-target activity confirmation via mechanism based G2/M escape assay was demonstrated. Physico-chemical and ADME properties were optimized to improve oral bioavailability in mouse.Entities:
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Year: 2012 PMID： 22632936 DOI： 10.1016/j.bmcl.2012.04.131
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823