Colchicine, an alkaloid extracted from the Colchicum autumnale plant, is a potent microtubule polymerization inhibitor both in vitro and in vivo. Although the parent molecule colchicine exhibits greatly high anticancer activity in vitro and in vivo, due to the high toxicity of colchicine, the use of colchicine has been limited. Previous studies have indicated that different modifications of colchicine enhance its anti-proliferative activity against several types of cancer cells. Thus, I study a series of triple-modified colchicine derivatives antitumor activity against a variety of cancer cells in vitro. There are three main possible results: (1) Triple-modified colchicine derivatives have better anti-proliferative activity against all cell lines than compound 1; (2) Triple-modified colchicine derivatives have better anti-proliferative activity against cancer cell lines than compound 1; (3) Triple-modified colchicine derivatives have better anti-proliferative activity against normal cell lines than compound Regardless of these results, further studies are going to focus on doing similar experiments in vivo and finding more effective drug inhibitors, as well as exploring the specific regulation mechanism of colchicine precisely.