Novel trimers of triphenylethylene-coumarin hybrid containing two amino side chains(5a-d and 6a-d)were designed and synthesized by the condensation of 1,3,5-benzenetricarboxylic acid with the varied amino monomeric hybrids catalyzed by HATU and DIPEA at room temperature.The extended trimeric compound 6a(R = piperidinyl) exhibited significant anti-proliferative activity against three cancer cells at IC_(50) of near 10μmol/L UV-vis,fluorescence(lifetime) and thermal denaturation exhibited that 6a had significant interaction with Ct-DNA by the intercalative mode of binding.The order of their antiproliferative activities was 6(a,d) > 5(a,d) and(5-6)a >(5-6)d,respectively,in accordance with that of their DNA binding properties,which suggested that the prolonged linker(six carbons) and piperidinyl group on the side chains are beneficial to DNA binding and the anti-tumor activity.
Li ZhangYu-Chao YaoMeng-Ying GaoRui-Xue RongKe-Rang WangXiao-Liu LiHua Chen
