Naparat KammasudChantana BoonyaratSatoshi TsunodaHiroaki SakuraiIkuo SaikiDavid S. GriersonOpa VajraguptaMahidol UniversityKhon Kaen UniversityInstitute of Natural MedicineCNRS Centre National de la Recherche Scientifique2018-08-242018-08-242007-09-01Bioorganic and Medicinal Chemistry Letters. Vol.17, No.17 (2007), 4812-48180960894X2-s2.0-34547498439https://repository.li.mahidol.ac.th/handle/123456789/24136NP603, the 6-dimethoxy phenyl indolin-2-one, was designed as FGF receptor 1 inhibitor by computational study. NP603 was synthesized and found to be more active against endothelial proliferation of HUVEC after the rhFGF-2 stimulation than SU6668 with minimum effective dose of 0.4 μM but with similar potency as SU16g. NP603 inhibited the tyrosine phosphorylation in FGF receptor and the activation of extracellular signal-regulated kinase and c-Jun-N-terminal-kinase after the rhFGF-2 stimulation. The increase in activity of NP603 supports the role of Lys514 movement in ligand-receptor binding in modeling study as the movement accommodates the hydrophobic interaction at the receptor pocket leading to the enhancement of binding capacity. © 2007 Elsevier Ltd. All rights reserved.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.bmcl.2007.06.058