Novel 2-amino-4-aryl-6-pyridopyrimidines and N-alkyl derivatives: Synthesis, characterization and investigation of anticancer, antibacterial activities and DNA/BSA binding affinities
作者:Nuran Kahriman、Kıvanç Peker、Vildan Serdaroğlu、Ali Aydın、Asu Usta、Seda Fandaklı、Nurettin Yaylı
DOI:10.1016/j.bioorg.2020.103805
日期:2020.6
2-amino-4-aryl-6-pyridopyrimidines (1-9) and their N-alkyl bromide derivatives (2a-c, 3a-c,5a-c,6a-c, 8a-c, 9a-c). Studies on the cells revealed that both pyrimidines and their alkyl derivatives (i) have a high anti-proliferative and anti-microbial activities, (ii) cause cell rounding, cytoplasmic blebs, and anomalous globular structure, and (iii) strongly bound to DNA/BSA macromolecules. Especially the
设计并合成了一系列新的2-氨基-4-芳基-6-吡啶并嘧啶及其N-烷基溴化物衍生物,方法是使用甲基取代的氮杂双氮杂环戊烯。对这些新型化合物进行了评估,并就其抗癌和抗微生物功能以及它们与DNA /蛋白质的结合亲和力与众所周知的化学疗法进行了比较。为了观察细胞增殖,细胞毒性和微稀释特性,用2-氨基-4-芳基-6-吡啶嘧啶(1-9)处理了多种癌细胞系(Hep3B,A549,HeLa,C6,HT29,MCF7)。 )及其N-烷基溴化物衍生物(2a-c,3a-c,5a-c,6a-c,8a-c,9a-c)。对细胞的研究表明,嘧啶及其烷基衍生物(i)具有很高的抗增殖和抗微生物活性,(ii)引起细胞变圆,细胞质起泡,球状结构异常;(iii)与DNA / BSA大分子牢固结合。尤其是N-烷基溴化物的烷基链的长度对抗增殖,抗菌和细胞毒性功能以及DNA /蛋白质结合亲和力具有增加的作用。这些结果表明该新化合物是有