Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors
作者:Liping Wang、Rong Wu、Wenwei Fu、Yuanzhi Lao、Changwu Zheng、Hongsheng Tan、Hongxi Xu
DOI:10.1016/j.bmc.2016.06.054
日期:2016.9
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,
最近发现,从云南藤黄的果实中分离出的一种多烯丙基化的苯甲酰间苯三酚天然产物(PPAP)之一,Oblongifolin C是一种有效的抗肿瘤剂。合成了对苯甲酮部分进行了修饰的12种衍生物的集合,并测试了其对c-Met激酶的抑制作用以及对HepG2,Miapaca-2,HCC827,Hela,A549,AGS和HT-29细胞系的细胞毒性。发现一种氧化的衍生物10在HCC827细胞系中具有强大的抑制和抗迁移特性,并作为开发新的抗癌药物的潜在先导化合物。此外,还评估了构效关系(SAR),为将来的抗癌药物开发提供关键信息。