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

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4507-11. doi: 10.1016/j.bmcl.2011.05.122.
Marina Caldarelli  1 ,  Mauro Angiolini ,  Teresa Disingrini ,  Daniele Donati ,  Marco Guanci ,  Stefano Nuvoloni ,  Helena Posteri ,  Francesca Quartieri ,  Marco Silvagni ,  Riccardo Colombo
Affiliations
  • 1. Nerviano Medical Sciences srl, Business Unit Oncology, Nerviano, MI, Italy. [email protected]
PMID: 21723120 DOI: 10.1016/j.bmcl.2011.05.122
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.