Design and Synthesis of 1,3,4-Thiadiazole Derivatives as Type IV Collagenase Inhibitors

作者：Chen Xiaolin; Wang Dongchao; Kuang Binhai; Li Shaohua; Tu Guogang^*

来源：Latin American Journal of Pharmacy, 2015, 34(9): 1772-1777.

• enzyme inhibitors
• MMP-2
• MMP-9
• synthesis
• type IV collagenase

Type IV collagenase is an essential metallopeptidase in the development of tumor invasion and angiogenesis. A series of novel low molecular-weight 1,3,4-thiadiazole derivatives were designed and synthesized as antitumor agents. The structures were confirmed by IR, H-1-NMR, and MS. Some of the target compounds display excellent potency toward MMP-2 and MMP-9 with inhibition rate > 50% at 10 mu M, meanwhile the selectivity towards MMP-9 is higher than towards MMP-2, and could be used as lead compounds for exploring new type IV collagenase inhibitors in the future.

• 出版日期2015-11
• 单位南昌大学