title: Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.
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.
authors: Nerviano Medical Sciences srl, Business Unit Oncology, Nerviano, MI, Italy. marina.caldarelli@nervianoms.com
authors: Marina
authors: M
authors: Caldarelli
authors: Mauro
authors: M
authors: Angiolini
authors: Teresa
authors: T
authors: Disingrini
authors: Daniele
authors: D
authors: Donati
authors: Marco
authors: M
authors: Guanci
authors: Stefano
authors: S
authors: Nuvoloni
authors: Helena
authors: H
authors: Posteri
authors: Francesca
authors: F
authors: Quartieri
authors: Marco
authors: M
authors: Silvagni
authors: Riccardo
authors: R
authors: Colombo
mesh_terms: D000284:Administration, Oral; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011505:Protein-Tyrosine Kinases; D011799:Quinazolines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D018797:Cell Cycle Proteins; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D011505:Protein-Tyrosine Kinases; D017346:Protein Serine-Threonine Kinases; C075840:TTK protein, human