Design, synthesis and biological evaluation of new ganglioside GM3 analogues as potential agents for cancer therapy.

Ganglioside GM3 is well known as a tumor-associated carbohydrate antigen on several types of tumors. Many studies have demonstrated that GM3 plays roles in cells proliferation, adhesion, motility and differentiation, which is involved in the process of cancer development. In the present study, we developed methods to synthesize GM3 analogues conveniently. By enzymatic hydrolysis and chemical procedures, two novel analogues and two known analogues were synthesized, containing lactose and glucosamine. Then anti-proliferation and anti-migration activities were evaluated by cytotoxicity assays and wound healing tests, and the data demonstrated that these analogues exhibited anticancer activities. Based on our previous studies, the structure-activity relationships were discussed. This study could provide valuable sight to find new antitumor agents for cancer therapy. Results exhibited that these analogues can inhibit cancer cell growth and migration. Image 1 • Two novel GM3 analogues containing lactose and glucosamine were synthesized. • GM3 analogues showed antitumor activities by cytotoxicity assays and wound healing tests. • This work provided valuable information to study carbohydrate derivatives as potential agents for cancer therapy. [ABSTRACT FROM AUTHOR]