Synthesis of dihydropyrazole sulphonamide derivatives that act as anti-cancer agents through COX-2 inhibition

For years now, COX-2 inhibitors have been used to treat pain and inflammation. Recently, much research has suggested that they may potentially be able to reduce tumour processes. COX-2 can be upregulated by tumor promotors, revealing that it may be involved in pathological processes of various types of cancer. Currently, there are hundreds of clinical trials being conduced testing the anti-tumor properties of COX-2 inhibitors such as celecoxib.

The investigators in this study created new COX-2 inhibitors derived from an analysis of currently known COX-2 inhibitors. One of the dihydropyrazole sulphonamide derivatives developed, 4d, demonstrated high COX-2 selectivity and anticancer properties. Further, it was shown that 4d could stop the cell cycle at the G2/M phase. It also induced apoptosis in A549 (tumor cell-line) cells. Overall, it seems that compound 4d could potentially be utilized for cancer treatment.

Qiu H, Wang P, Zhen L, et al. Synthesis of dihydropyrazole sulphonamide derivatives that act as anti-cancer agents through COX-2 inhibition. Pharmacol Res. 2016;104:86-96.

 

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