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

MG Bursavich, D Dastrup, M Shenderovich…

Index: Bursavich, Matthew G.; Dastrup, David; Shenderovich, Mark; Yager, Kraig M.; Cimbora, Daniel M.; Williams, Brandi; Kumar, D. Vijay Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6829 - 6833

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Citation Number: 9

Abstract

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 ...