Pyridylmethylthio derivatives as VEGF inhibitors. Part 1

  • Bioorg Med Chem Lett. 2010 Dec 15;20(24):7234-8. doi: 10.1016/j.bmcl.2010.10.096.
Hisashi Tajima  1 ,  Takahiro Honda ,  Kenji Kawashima ,  Yoshimasa Sasabuchi ,  Minoru Yamamoto ,  Masakazu Ban ,  Kazuyoshi Okamoto ,  Kenji Inoue ,  Takaaki Inaba ,  Yuriko Takeno ,  Hiroyuki Aono
Affiliations
  • 1. Research and Development Center, Santen Pharmaceutical Co. Ltd, Ikoma-shi, Nara, Japan. [email protected]
PMID: 21074435 DOI: 10.1016/j.bmcl.2010.10.096
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).