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Bioorg Med Chem Lett. 2013 Dec 15;23(24):6829-33. doi: 10.1016/j.bmcl.2013.10.008. Epub 2013 Oct 11.

Novel Mps1 kinase inhibitors: from purine to pyrrolopyrimidine and quinazoline leads.

Author information

1
Medicinal Chemistry, Myrexis, Inc., 305 Chipeta Way, Salt Lake City, UT 84108, United States. Electronic address: mbursavich@envivopharma.com.

Abstract

Mps1, also known as TTK, is a mitotic checkpoint protein kinase that has become a promising new target of cancer research. In an effort to improve the lead-likeness of our recent Mps1 purine lead compounds, a scaffold hopping exercise has been undertaken. Structure-based design, principles of conformational restriction, and subsequent scaffold hopping has led to novel pyrrolopyrimidine and quinazoline Mps1 inhibitors. These new single-digit nanomolar leads provide the basis for developing potent, novel Mps1 inhibitors with improved drug-like properties.

KEYWORDS:

Cancer; Conformational restriction; Mps1; Protein kinase inhibitors; Purines; Pyrrolopyrimidines; Quinazoline; Scaffold hopping; Structure-based design; TTK

PMID:
24183538
DOI:
10.1016/j.bmcl.2013.10.008
[Indexed for MEDLINE]
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