摘要
A series of novel uracil and 5-fluorouracil-l-yl-acetic acid-colchicine derivatives（6a--6n） was synthe- sized via coupling and 5-fluorouracil（5-FU） with C-10 analogues of colchicine. The antitumor activities of the target compounds against human hepatocellular earcinoma（BEL7402） cells, human ovary carcinoma（A2780） cells, human lung adenocarcinoma（A549） cells and human breast carcinoma（MCF7） cells were tested in vitro, and the structure-activity relationship（SAR） of the compounds was also studied. The bioassay results demonstrate that most of the tested compounds display significant activity and particularly, compounds 6a, 6e, 6h and 61 show more potent cytotoxic activities than 5-fluorouracil and colchicine. The results show that the new derivatives of colchicine are potential suppressors on human cancer.
Abstract A series of novel uracil and 5-fluorouracil-l-yl-acetic acid-colchicine derivatives（6a--6n） was synthe- sized via coupling and 5-fluorouracil（5-FU） with C-10 analogues of colchicine. The antitumor activities of the target compounds against human hepatocellular earcinoma（BEL7402） cells, human ovary carcinoma（A2780） cells, human lung adenocarcinoma（A549） cells and human breast carcinoma（MCF7） cells were tested in vitro, and the structure-activity relationship（SAR） of the compounds was also studied. The bioassay results demonstrate that most of the tested compounds display significant activity and particularly, compounds 6a, 6e, 6h and 61 show more potent cytotoxic activities than 5-fluorouracil and colchicine. The results show that the new derivatives of colchicine are potential suppressors on human cancer.
