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Bioorg Med Chem Lett. 2012 Jul 1;22(13):4377-85. doi: 10.1016/j.bmcl.2012.04.131. Epub 2012 May 5.

Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.

Author information

1
Department of Medicinal Chemistry, Myrexis Inc., 305 Chipeta Way, Salt Lake City, UT 84108, USA. dvijayku@hotmail.com

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.

PMID:
22632936
DOI:
10.1016/j.bmcl.2012.04.131
[Indexed for MEDLINE]

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