Yurttaş Leyla, Demirayak Seref, Ilgın Sinem, Atlı Özlem
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Turkey.
Department of Pharmaceutical Chemistry, School of Pharmacy, Medipol University, 34083 Istanbul, Turkey.
Bioorg Med Chem. 2014 Nov 15;22(22):6313-23. doi: 10.1016/j.bmc.2014.10.002. Epub 2014 Oct 13.
A series of 1,2,4-triazine derivatives bearing piperazine amide moiety has been synthesized and investigated for their potential anticancer activities. 1-[4-(5,6-Bis(4-subtituted phenyl)-1,2,4-triazin-3-yl)piperazin-1-yl]-2-[4-(3-substituted phenyl)piperazin-1-yl]ethanone derivative (1-32) compounds were synthesized by a four step synthetic procedure. The activity studies were evaluated using XTT method, BrdU method and flow cytometric analysis on MCF-7 breast cancer cells and NIH/3T3 (mouse embryonic fibroblast cells) healthy cells. Compounds 5 with 3-chlorophenyl and compound 7 with 4-chlorophenyl substitutions were found to be promising antiproliferative agents comparing with an effective anticancer drug, cisplatin.
一系列带有哌嗪酰胺部分的1,2,4-三嗪衍生物已被合成，并对其潜在的抗癌活性进行了研究。1-[4-(5,6-双(4-取代苯基)-1,2,4-三嗪-3-基)哌嗪-1-基]-2-[4-(3-取代苯基)哌嗪-1-基]乙酮衍生物(1-32)化合物通过四步合成程序合成。使用XTT法、BrdU法和流式细胞术分析对MCF-7乳腺癌细胞和NIH/3T3(小鼠胚胎成纤维细胞)健康细胞进行活性研究。与有效的抗癌药物顺铂相比，发现具有3-氯苯基取代的化合物5和具有4-氯苯基取代的化合物7是有前景的抗增殖剂。
