Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp

  • J Nat Prod. 2013 Apr 26;76(4):715-9. doi: 10.1021/np300535c.
Chisato Nosaka  1 ,  Hayamitsu Adachi ,  Ryuichi Sawa ,  Koichi Nakae ,  Sonoko Atsumi ,  Naoko Kinoshita ,  Yumiko Kubota ,  Masayuki Igarashi ,  Yoshihisa Sei ,  Kentaro Yamaguchi ,  Masabumi Shibuya ,  Yoshio Nishimura ,  Yuzuru Akamatsu
Affiliations
  • 1. Institute of Microbial Chemistry (BIKAKEN), Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
PMID: 23414235 DOI: 10.1021/np300535c
Abstract

A new inhibitor of VEGF Receptor Tyrosine Kinases, vegfrecine (1), was isolated from the culture broth of Streptomyces sp. MK931-CF8. The molecular structure of 1 was determined by NMR and MS analysis combined with synthesis. Compound 1 showed potent inhibitory activity against vascular endothelial growth factor receptor (VEGFR) tyrosine kinases in in vitro enzyme assays, but platelet-derived growth factor receptors (PDGFRs), Fibroblast Growth Factor receptor (FGFR), and epidermal growth factor receptor (EGFR) responded only weakly. Compound 1 is a promising new selective VEGFR Inhibitor for investigating new treatments of Cancer and inflammatory diseases.