Synthesis and Cytotoxic Evaluation of Novel Symmetrical Taspine Derivatives as Anticancer Agents

Jie      Zhang; Yanmin      Zhang; Xiaoyan      Pan; Sicen      Wang; Langchong      He

doi:10.2174/157340611796150914

Abstract

It has been demonstrated that taspine derivatives act as anticancer agents, thus we designed and synthesized a novel class of symmetrical biphenyl derivatives. We evaluated the cytotoxicity and antitumor activity of biphenyls against five human tumor and normal cell lines. The results indicated that the majority of the compounds exhibited anticancer activity equivalent to or greater than the positive control. Compounds (11) and (12) demonstrated the most potent cytotoxic activity with IC50 values between 19.41 μM and 29.27 μM. The potent antiproliferative capabilities of these compounds against ECV304 human transformed endothelial cells indicated that these biphenyls could potentially serve as antiangiogenic agents. We also reviewed the relationship between structure and activity based on the experimental results. Our findings provide a good starting point for further development of symmetrical biphenyl derivatives as potential novel anticancer agents.

Keywords: Symmetrical taspine derivatives, antiproliferative activity, cytotoxicity, anticancer agents, antiangiogenic agents, VEGFR-2, biphenyl derivatives, antitumor, IC50, endothelial cells, structure and activity