Facile Synthesis and Biological Evaluation of Novel Symmetrical Biphenyls as Antitumor Agents

Jie Zhang, Yanmin Zhang, Xiaoyan Pan, Chen Wang, Zhigang Hu, Sicen Wang, Langchong He

doi:10.2174/157340612800493656

Abstract

As a continuation to our previous work in developing anticancer agents, eighteen symmetrical biphenyl derivatives structurally related to taspine were synthesized and evaluated in vitro and in vivo. All the compounds were prepared with varied substitutions in the phenyl ring of aniline moiety. The cytotoxicity and anticancer activity of biphenyls was evaluated against various human tumor and normal cell line. Antiproliferative assays indicated that some of them exhibited potent anticancer activity. The potent antiproliferative activity of these compounds against ECV304 suggested that these biphenyls could be served as antiangiogenic agents. The highly active compound (2) also exhibited potent growth inhibition against cancer cell lines in vivo. Our findings demonstrated that these symmetrical biphenyl derivatives would be a promising candidate as novel anticancer agents.

Keywords: Symmetrical biphenyls, Antiproliferative activity, Cytotoxicity, Antitumor agents, VEGFR-2, antiangiogenic agents, Antiproliferative, biphenyls, Antitumor, Chemotherapy