Pyridylmethylthio derivatives as VEGF inhibitors: part 2

  • Bioorg Med Chem Lett. 2011 Feb 15;21(4):1232-5. doi: 10.1016/j.bmcl.2010.12.071.
Hisashi Tajima  1 ,  Takahiro Honda ,  Kenji Kawashima ,  Yoshimasa Sasabuchi ,  Minoru Yamamoto ,  Masakazu Ban ,  Kazuyoshi Okamoto ,  Kenji Inoue ,  Takaaki Inaba ,  Yuriko Takeno ,  Takashi Tsuboi ,  Asaka Tonouchi ,  Hiroyuki Aono
Affiliations
  • 1. Research and Development Center, Santen Pharmaceutical Co. Ltd, 8916-16 Takayama-cho Ikoma-shi, Nara 630-0101, Japan. [email protected]
PMID: 21247763 DOI: 10.1016/j.bmcl.2010.12.071
Abstract

Optimization of compounds 5 and 6 led to the discovery of VEGF inhibitor 10g which reduced CYP inhibition. It was highly active in vitro (VEGF induced HUVEC proliferation assay) and showed efficacies in three disease models in vivo (Cancer, RA, and AMD).