An alpha(1)-adrenergic receptor ligand repurposed as a potent antiproliferative agent for head and neck squamous cell carcinoma

作者：Zagni Chiara; Guimaraes Douglas Magno; Salerno Loredana; Punzo Francesco; Squarize Cristiane H; Mineo Placido Giuseppe; Romeo Giuseppe^*; Rescifina Antonio

来源：RSC Advances, 2015, 5(9): 6536-6542.

DOI：10.1039/c4ra11856a

In this study we report the anticancer properties of RN5-Me, an alpha(1)-adrenergic receptor ligand. Biological screening and circular dichroism data indicate that it acts as a DNA intercalator. Docking studies, confirming this behaviour, suggest that RN5-Me possesses great selectivity for alternating AT nucleobases upon GC ones. In the cytotoxicity assay, it shows IC50 values in the range of 4.2-25.0 nM towards the cancer cell lines HN6, HN13, HeLa, SK-Me1-103, PC3, and MCF7. It is noteworthy that RN5-Me shows a higher selectivity than Cisplatin for HN6 and HN13 over NOK-SI non-cancerous cells.

• 出版日期2015