N-取代二吡啶甲基胺锌配合物的合成、与DNA作用和抗肿瘤活性

本文以N-烯丙基二吡啶甲基胺(Aldpa)和2,2-二(2-吡啶甲胺基)丙酸(Adpa)为配体,合成了2个锌配合物,并运用IR,UV,ES-MS等方法进行了表征.X-衍射晶体结构表明(Adpa)Zn(CHCOO)]配合物中锌(Ⅱ)离子采取五配位三角双锥构型.紫外和荧光光谱滴定研究结果显示(Adpa)Zn(CHCOO)]与ctDNA作用强于(Aldpa)ZnCl2].用MTT法研究了配合物体外对肿瘤细胞生长的抑制作用.实验结果表明与ctDNA作用强的锌配合物抗肿瘤活性较好,二吡啶甲基胺氮原子上的取代基影响相应锌(Ⅱ)配合物的抗肿瘤活性.

Synthesis, Interaction with DNA and Antitumor Activities of Zinc(Ⅱ) Complexes with N-substituted Di(picolyl)amines

Two Zn(Ⅱ) complexes with Allyl bis(2-pyridylmethyl)amine (Aldpa), or bis(2-pyridylmethyl)amino-2-propionate(Adpa), were synthesized and characterized by IR, UV, ES-MS. The crystal structure shows that the Zn(Ⅱ) ion in (Adpa)Zn(CHCOO)] is coordinated by three N atoms, one oxygen atom of the Adpa and one oxygen atom of CH3COO-, forming a distorted trigonal bipyramidal geometry. The spectrophotometric and fluorescence titration data indicate that the interaction between the (Adpa)Zn(CHCOO)] with ct-DNA is more stronger than that of (Aldpa)ZnCl2]. The (Adpa)Zn(CH3COO)] is more active against the four cancer cells (Mcf-7, Eca-109, A549, Hela) than the (Aldpa)ZnCl], indicating the antitumor activity of zinc(Ⅱ) complexes is dependent on its binding to DNA. The bioassay results also show that the substituents introduced on the secondary amino nitrogen atom of dpa have great contribution to the antitumor activities of these zinc(Ⅱ) complexes. Information obtained from the present is helpful to development of therapeutic agents. CCDC: 709681.