| Literature DB >> 15771417 |
Nand Baindur1, Naresh Chadha, Benjamin M Brandt, Davoud Asgari, Raymond J Patch, Celine Schalk-Hihi, Theodore E Carver, Ioanna P Petrounia, Christian A Baumann, Heidi Ott, Carl Manthey, Barry A Springer, Mark R Player.
Abstract
2-Hydroxy-4,6-diamino-[1,3,5]triazines are described which are a novel class of potent inhibitors of the VEGF-R2 (flk-1/KDR) tyrosine kinase. 4-(Benzothiazol-6-ylamino)-6-(benzyl-isopropyl-amino)-[1,3,5]triazin-2-ol (14d) exhibited low nanomolar potency in the in vitro enzyme inhibition assay (IC(50) = 18 nM) and submicromolar inhibitory activity in a KDR-induced MAP kinase autophosphorylation assay in HUVEC cells (IC(50) = 280 nM), and also demonstrated good in vitro selectivity against a panel of growth factor receptor tyrosine kinases. Further, 14d showed antiangiogenic activity in an aortic ring explant assay by blocking endothelial outgrowths in rat aortas with an IC(50) of 1 microM.Entities:
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Year: 2005 PMID： 15771417 DOI： 10.1021/jm049372z
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446