Vegfrecine, an Inhibitor of VEGF Receptor Tyrosine Kinases Isolated from the Culture Broth of Streptomyces sp.

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• 作者：Chisato Nosaka ; Hayamitsu Adachi ; Ryuichi Sawa ; Koichi Nakae ; Sonoko Atsumi ; Naoko Kinoshita ; Yumiko Kubota ; Masayuki Igarashi ; Yoshihisa Sei ; Kentaro Yamaguchi ; Masabumi Shibuya ; Yoshio Nishimura ; Yuzuru Akamatsu
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：April 26, 2013
• 年：2013
• 卷：76
• 期：4
• 页码：715-719
• 全文大小：261K
• 年卷期：v.76,no.4(April 26, 2013)
• ISSN：1520-6025

文摘

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.