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Title: 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases
Authors: Naparat Kammasud
Chantana Boonyarat
Kingkan Sanphanya
Maleeruk Utsintong
Satoshi Tsunoda
Hiroaki Sakurai
Ikuo Saiki
Isabelle André
David S. Grierson
Opa Vajragupta
Mahidol University
Khon Kaen University
Institute of Natural Medicine
CNRS Centre National de la Recherche Scientifique
Keywords: Biochemistry, Genetics and Molecular Biology;Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Feb-2009
Citation: Bioorganic and Medicinal Chemistry Letters. Vol.19, No.3 (2009), 745-750
Abstract: NP506, the 3-{2,4-dimethyl-5-[2-oxo-5-(N′-phenylhydrazinocarbonyl)-1,2-dihydro-indol-3-ylidenemethyl]-1H-pyrrol-3-yl}-propionic acid, was designed as FGF receptor 1 inhibitor by computational study and found to be more active against endothelial proliferation of HUVEC after the rhFGF-2 stimulation than SU6668 with minimum effective dose of 10 μM. NP506 inhibited the tyrosine phosphorylation in FGF, VEGF, and PDGF receptors and the activation of extracellular signal-regulated kinase (ERK), c-Jun-N-terminal-kinase (JNK) and AKT after the rhFGF-2 stimulation. The introduction of the phenyl hydrazide motif to the position 5 of the pyrido[2,3-d]pyrimidine scaffold led to the inhibitory effect in two signaling pathways: inhibition of AKT activation in the phosphatidyl inositol 3′-kinase (PI13K)/AKT signaling pathway and the inhibition of ERK and JNK activation in MAPK pathway. © 2008 Elsevier Ltd. All rights reserved.
ISSN: 0960894X
Appears in Collections:Scopus 2006-2010

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