Design, Hemiysnthesis, crystal structure and anticancer activity of 1, 2, 3-triazoles derivatives of totarol
Résumé
A new series of diverse triazoles linked to the hydroxyl group of totarol were synthesized using click chemistry approach. The structure of these compounds was elucidated by HRMS, IR and NMR spectroscopy. The structure of compound 3g was also confirmed by x-ray single crystal diffraction. The cytotoxicity of these compounds was evaluated by the MTT method against four cancer cell lines, including fibrosarcoma HT-1080, lung carcinoma A-549, and breast adenocarcinoma (MDA-MB-231 and MCF-7), and the results indicated that all compounds showed weak to moderate activities against all cancer cell lines ,with IC50 values ranging from 14.44 to 46.25 μM. On the basis of our research the structure-activity relationships (SAR) of these compounds were discussed. This work provides some important hints for further structural modification of totarol towards developing novel and highly effective anticancer drugs. Respectively. It is interesting to note that the compound 3g indicated a very significant cytotoxicity against HT-1080 and A-549 cell lines.
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