Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 138, Issue -, Pages 1076-1088Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.07.011
Keywords
5,6-Diaryl-1,2,4-triazines; Molecular hybridization strategy; Morphological changes; Apoptosis; Apoptosis-related proteins
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Funding
- National Natural Sciences Foundations of China [81673322, 81273393, 81430085, 21372206, 81172937]
- Ministry of Education [20134101130001]
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A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) for these 5,6-diaryl-1,2,4-triazines is explored in this report with evaluation of 15 variants of the structural class. Among these chemical derivatives, 3-(((1-(4-fluorobenzy1)-1H-1,2,3-triazol-4-yl)methyl)thio)-5,6-dipheny1-1,2,4-triazine(11E) showed the more potent inhibitory effect against three cell lines than 5-Fu. Cellular mechanism studies in MGC-803 cells elucidated 11E inhibited colony formation and arrested cell cycle at G2/M phase. Furthermore, compound 11E caused morphological changes, decreased mitochondrial membrane potential, and induced apoptosis through the apoptosis-related proteins in MGC-803 cells. It was the first time, to our knowledge, that 5,6-diaryl-1,2,4-triazines bearing a 1,2,3-triazole linker were used as potential apoptosis inducers. (C) 2017 Elsevier Masson SAS. All rights reserved.
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