| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596636 | Bioorganic & Medicinal Chemistry Letters | 2012 | 9 Pages |
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.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
D. Vijay Kumar, 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,