Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors. Issue 18 (15th September 2016)

• Record Type: Journal Article
• Authors: Wang, Liping; Wu, Rong; Fu, Wenwei; Lao, Yuanzhi; Zheng, Changwu; Tan, Hongsheng; Xu, Hongxi
• Is Part Of: Bioorganic & medicinal chemistry. Volume 24:Issue 18(2016)
• Page Start: 4120
• Page End: 4128
• Publication Date: 2016-09-15
• Subjects: Oblongifolin C -- Modification -- Derivatives -- c-Met kinase inhibitor -- Cytotoxicity -- HCC827 cell line -- Structure–activity relationships; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2016.06.054
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Oblongifolin C, one of the polyprenylated benzoylphloroglucinol natural products (PPAPs) isolated from the fruits of Garcinia yunnanensis Hu, was recently discovered to be a potent anti-tumor agent. A collection of 12 derivatives with modifications on the benzophenone moieties were synthesized and tested for c-Met kinase inhibition and cytotoxicity against the HepG2, Miapaca-2, HCC827, Hela, A549, AGS, and HT-29 cell lines in vitro. An oxidized derivative, 10, was found to possess strong inhibition and anti-migration properties in the HCC827 cell line and serves as a potential lead compound for the development of new anticancer drugs. In addition, structure–activity relationships (SAR) were also evaluated to provide key information for future anticancer drug development.