5-氟尿嘧啶-1-烷氧苯基三间氯苯基卟啉的合成及其体外抗癌活性

Synthesis and Antitumor Activity in Vitro of 5-Fluorouracil-1-alkylaxgphenyl-tetra m-Chlorophenyl Porphyrin Compounds

为提高5-氟尿嘧啶抗癌的靶向性,降低其不良反应,合成了5种新型卟啉-5-氟尿嘧啶衍生物及其Mn3+配合物,优化了合成反应条件,探索了目标化合物的分离方法。通过IR、UV-Vis、1H NMR和ESI-MS对化合物结构和组成进行了确认。采用四甲基偶氮唑蓝(MTT)比色法,以5-氟尿嘧啶为阳性对照药,测试了卟啉化合物对5种肿瘤细胞的体外抑制活性。初筛结果显示,化合物D3对人卵巢癌细胞Sk-ov-3有较强的抑制作用。

To search for more potential antitumor agents, five new porphyrin-5-fluorouracil compounds were designed and synthesized. The reaction conditions were optimized and the separation method of the target products was explored. The compositions and structures of these compounds were confirmed by IR, UV-Vis, 1H NMR and MS. Their cytotoxicity against five human cancer cell lines in vitro was evaluated by MTI＂ assay. Biological screening results demonstrate that some tested compounds exhibit potential antitumor activity, particularly, compound D3 shows more potential cytotoxic activities than the control 5-fluorouracil against Sk-ov-3 cells.