Ratchanok PingaewSupaluk PrachayasittikulSomsak RuchirawatVirapong PrachayasittikulSrinakharinwirot UniversityMahidol UniversityChulabhorn Research InstituteChulabhorn Graduate InstituteThailand Ministry of Education2018-11-092018-11-092014-01-01Medicinal Chemistry Research. Vol.23, No.4 (2014), 1768-178015548120105425232-s2.0-84899410430https://repository.li.mahidol.ac.th/handle/20.500.14594/33669A new series of 4-(4-(substituted)-1H-1,2,3-triazol-1-yl)-N- phenethylbenzenesulfonamide derivatives 5 were synthesized through the Click approach and evaluated for their cytotoxic activity against four cancer cell lines (HuCCA-1, HepG2, A549, and MOLT-3). Most of the synthesized triazoles 5 displayed cytotoxicity against MOLT-3 cell line, except for analogs 5a-c and 5e. Significantly, 4-phenyltriazoles (5a and 5n), 4-(naphthalen-2-yloxy) methyltriazole 5d, as well as 4-((2-oxo-2H-chromen-7-yl)oxy)methyltriazole 5l showed higher cytotoxic activity against HepG2 cells than the reference drug, etoposide. Interestingly, the 4-phenyltriazole 5a was the most potent and promising compound with IC50value of 9.07 μM against HepG2 cell line. The analog 5a also exerted the highest cytotoxic activity against HuCCA-1 cells. This finding provides the novel lead molecules for further development. © Springer Science+Business Media 2013.Mahidol UniversityChemistryPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1007/s00044-013-0777-z