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Bioorg Med Chem Lett. 2011 Aug 1;21(15):4507-11. doi: 10.1016/j.bmcl.2011.05.122. Epub 2011 Jun 14.

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.

Author information

1
Nerviano Medical Sciences srl, Business Unit Oncology, Nerviano, MI, Italy. marina.caldarelli@nervianoms.com

Abstract

The synthesis and SAR of a series of novel pyrazolo-quinazolines as potent and selective MPS1 inhibitors are reported. We describe the optimization of the initial hit, identified by screening the internal library collection, into an orally available, potent and selective MPS1 inhibitor.

PMID:
21723120
DOI:
10.1016/j.bmcl.2011.05.122
[Indexed for MEDLINE]

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