Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593359 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Matthew G. Bursavich, David Dastrup, Mark Shenderovich, Kraig M. Yager, Daniel M. Cimbora, Brandi Williams, D. Vijay Kumar,