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 ...

533-30-2

6-Aminobenzothiazole

~51%

Synthesis and evaluation of three 18F-labeled aminophenylben...

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Mesolimbic selective antipsychotic arylcarbamates

[Hansen, John Bondo; Fink-Jensen, Anders; Christensen, Birgitte V.; Gronvald, Frederick C.; Jeppesen, Lone; Mogensen, John P.; Nielsen, Erik B.; Scheideler, Mark A.; White, Francis J.; Zhang, Xu-Feng European Journal of Medicinal Chemistry, 1998 , vol. 33, # 11 p. 839 - 858]

Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridy...

[Swahn, Britt-Marie; Wensbo, David; Sandell, Johan; Sohn, Daniel; Slivo, Can; Pyring, David; Malmstroem, Jonas; Arzel, Erwan; Vallin, Michaela; Bergh, Margareta; Jeppsson, Fredrik; Johnson, Allan E.; Jureus, Anders; Neelissen, Jan; Svensson, Samuel Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 6 p. 1976 - 1980]