title: Pyridylmethylthio derivatives as VEGF inhibitors. Part 1.
abstract: Optimization from compound 4a, having intramolecular S-O nonbonded interaction, led to discover compounds 4m and 4n. They were highly active in vitro (VEGF induced HUVEC proliferation assay) and showed efficacies in three disease models in vivo (cancer, RA, AMD).
authors.affiliation: Research and Development Center, Santen Pharmaceutical Co. Ltd, Ikoma-shi, Nara, Japan. hisashi.tajima@santen.co.jp
authors.forename: Hisashi
authors.initials: H
authors.lastname: Tajima
authors.forename: Takahiro
authors.initials: T
authors.lastname: Honda
authors.forename: Kenji
authors.initials: K
authors.lastname: Kawashima
authors.forename: Yoshimasa
authors.initials: Y
authors.lastname: Sasabuchi
authors.forename: Minoru
authors.initials: M
authors.lastname: Yamamoto
authors.forename: Masakazu
authors.initials: M
authors.lastname: Ban
authors.forename: Kazuyoshi
authors.initials: K
authors.lastname: Okamoto
authors.forename: Kenji
authors.initials: K
authors.lastname: Inoue
authors.forename: Takaaki
authors.initials: T
authors.lastname: Inaba
authors.forename: Yuriko
authors.initials: Y
authors.lastname: Takeno
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Aono
mesh_terms: D000813:Anilides / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D000818:Animals; D001169:Arthritis, Experimental / Q000188:drug therapy; D002460:Cell Line; D020256:Choroidal Neovascularization / Q000188:drug therapy; D004195:Disease Models, Animal; D042783:Endothelial Cells / Q000166:cytology; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors* / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
chemical_list: D000813:Anilides; D011725:Pyridines; D042461:Vascular Endothelial Growth Factor A; C023666:pyridine