N-烷基-1,10-菲咯啉2-甲胺La(Ⅲ)配合物的合成及抗癌活性

Synthesis and Antitumor Activity of Lanthanum(Ⅲ) Complexes to N-Alkyl-1,10-phenanthroline-2-methanamine

合成和表征了甲基、乙基、丙基、丁基和苄基N-取代1,10-菲咯啉2-甲胺衍生配体及其镧(Ⅲ)配合物.研究了配合物对HL60人白血病、PC-3MIE8人前列腺癌、BGC-823人胃癌、MDA-MB-435人乳腺癌、Bel-7402人肝癌、Hela人宫颈癌共6种瘤株的体外抗肿瘤活性及其与DNA的作用方式.结果表明,该系列化合物对实验的6种瘤株均具有不同程度的生长抑制作用,其中配合物L5LaL5对MDA-MB-435人乳腺癌和Bel-7402人肝癌的抑制效果较好,对Bel-7402人肝癌和Hela人宫颈癌的抑制效果优于顺铂.其作用机理可能是配合物以部分插入方式同时伴随共价和静电与DNA发生作用,影响其基因调控与表达,进而抑制肿瘤细胞的生长,最终导致癌细胞凋亡.

Five lathanum（ Ⅲ ） complexes containing 1,10-phenanthroline units were synthesized and characterized by elemental analyses, ^1 H HMR and IR spectra. All complexes were assayed for antitumor activity in vitro against HL-60（human leukocytoma） cells, PC-3MIE8（human prostate carcinoma） cells, BGC-823（human stomach carcinoma） cells, MDA-MB-435 （human galactophore carcinoma） cells, Bel-7402 （human liver carcinoma） cells and Hela（ human cervix carcinoma） cells. The results show that the complexes exhibit good growth inhibition against different cell lines in general. DNA binding studies indicate that the complexes possibly interact with ctDNA by part intercalative, covalent binding and electrostatic effection.