2-Hydroxy-4, 6-diamino-[1, 3, 5] triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors

…, C Schalk-HiHi, TE Carver, IP Petrounia…

Index: Baindur, Nand; Chadha, Naresh; Brandt, Benjamin M.; Asgari, Davoud; Patch, Raymond J.; Schalk-HiHi, Celine; Carver, Theodore E.; Petrounia, Ioanna P.; Baumann, Christian A.; Ott, Heidi; Manthey, Carl; Springer, Barry A.; Player, Mark R. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1717 - 1720

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Citation Number: 50

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 (IC50= 18 nM) and submicromolar inhibitory activity in a KDR- induced MAP kinase autophosphorylation assay in HUVEC cells (IC50= 280 nM), and ...

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