含三氟甲基或3,4,5-三甲氧基二苯乙烯腈衍生物的制备及其活性研究

以4-三氟甲基苯甲酸和3,4,5-三甲氧基苯甲酸为原料合成出2-(4-(三氟甲基)苯基)乙腈和2-(3,4,5-三甲氧基苯基)乙腈,将其作为中间体和几种醛类合成一系列含4-三氟甲基及3,4,5-三甲氧基二苯乙烯腈衍生物。所合成的化合物通过氢谱、碳谱与高分辨质谱进行表征后用MTT法在12种细胞上测得其细胞增殖抑制率,其中(Z)-3-(4-丙氧基苯基)-2-(3,4,5-三甲氧基苯基)丙烯腈显示最好的抗癌活性及选择性抑制活性,经进一步研究发现通过抑制细胞迁移与抑制集落形成达到抗癌效果,具有进一步开发研究的价值。

Synthesis and Pharmacological Evaluation of Diphenylacrylonitrile-bearing Trifluoromethyl or 3,4,5-Trimethoxy Group(s)

Intermediates 2-(4-(trifluoromethyl)phenyl)acetonitrile and 2-(3,4,5-trimethoxyphenyl)acetonitrile were synthesized using 4-(trifluoromethyl)benzoic acid and 3,4,5-trimethoxybenzoic acid as the starting materials respectively.Then reacted with kinds of aldehyde to synthesize a series of diphenylacrylonitrile-bearing trifluoromethyl or 3,4,5-trimethoxy group(s),and then confirmed with 1HNMR,13CNMR and HRMS and the anti-proliferatory activities were evaluated by MTT assay against 12 cell lines.The results indicated that(Z)-3-(4-propoxyphenyl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile expressed the best anti-tumor activity and the best selectivity.Further studies have shown that it achieved anti-tumor activity by inhibiting cell migration and colony-formation with treatment,and has further development value.