THE SYNTHESIS AND SAR OF NEW -(N-ALKYL-N-PHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINES AND 4-(N-ALKYL-N-PHENYL)AMINOPYRAZOLO [3,4-D]PYRIMIDINES, INHIBITORS OF CSF-1R TYROSINE KINASE-ACTIVITY

Authors
MYERS MR SETZER NN SPADA AP PERSONS PE LY CQ MAGUIRE MP ZULLI AL CHENEY DL ZILBERSTEIN A JOHNSON SE FRANKS CF MITCHELL KJ
Citation
Mr. Myers et al., THE SYNTHESIS AND SAR OF NEW -(N-ALKYL-N-PHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINES AND 4-(N-ALKYL-N-PHENYL)AMINOPYRAZOLO [3,4-D]PYRIMIDINES, INHIBITORS OF CSF-1R TYROSINE KINASE-ACTIVITY, Bioorganic & medicinal chemistry letters, 7(4), 1997, pp. 421-424
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
4
Year of publication
1997
Pages
421 - 424
Database
ISI
SICI code
0960-894X(1997)7:4<421:TSASON>2.0.ZU;2-F
Abstract
We have identified moderately potent and selective inhibitors of CSF-I R tyrosine kinase activity.(1) A preliminary SAR study resulted in the identification of compounds 11 and 20 as the most potent analogues in the series (IC50 = 0.18 mu M). The 3D-conformation of the 4-(N-alkyl- N-phenyl)-aminoquinazolines has been proposed to be important to the o verall selectivity and activity. (C) 1997, Elsevier Science Ltd.