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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Caldarelli M,Angiolini M,Disingrini T,Donati D,Guanci M,Nuvoloni S,Posteri H,Quartieri F,Silvagni M,Colombo R

doi

10.1016/j.bmcl.2011.05.122

subject

Has Abstract

pub_date

2011-08-01 00:00:00

pages

4507-11

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00763-3

journal_volume

21

pub_type

杂志文章

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