445268-54-2Relevant academic research and scientific papers
Novel thienopyridine derivatives as specific anti-hepatocellular carcinoma (HCC) agents: Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation
Zeng, Xiu-Xiu,Zheng, Ren-Lin,Zhou, Tian,He, Hai-Yun,Liu, Ji-Yan,Zheng, Yu,Tong, Ai-Ping,Xiang, Ming-Li,Song, Xiang-Rong,Yang, Sheng-Yong,Yu, Luo-Ting,Wei, Yu-Quan,Zhao, Ying-Lan,Yang, Li
supporting information; experimental part, p. 6282 - 6285 (2010/12/18)
Novel thienopyridine derivatives 1b-1r were synthesized, based on a hit compound 1a that was found in a previous cell-based screening of anticancer drugs. Compounds 1a-1r have the following features: (1) their anticancer activity in vitro was first reported by our group. (2) The most potent analog 1g possesses hepatocellular carcinoma (HCC)-specific anticancer activity. It can specifically inhibit the proliferation of the human hepatoma HepG2 cells with an IC50 value of 0.016 μM (compared with doxorubicin as a positive control, whose IC50 was 0.37 μM). It is inactive toward a panel of five different types of human cancer cell lines. (3) Compound 1g remarkably induces G0/G1 arrest and apoptosis in HepG2 cells in vitro at low micromolar concentrations. These results, especially the HCC-specific anticancer activity of 1g, suggest their potential in targeted chemotherapy for HCC.
