1620988-84-2Relevant articles and documents
One-pot synthesis and antiproliferative activity of novel 2,4-diaminopyrimidine derivatives bearing piperidine and piperazine moieties
Ma, Wei-Feng,Yang, Hai-Kui,Hu, Meng-Jin,Li, Qian,Ma, Tian-Zhu,Zhou, Zhong-Zhen,Liu, Rui-Yuan,You, Wen-Wei,Zhao, Pei-Liang
, p. 127 - 134 (2014/07/22)
A series of novel 2,4-diaminopyrimidines containing piperidine and piperazine moieties were synthesized via an efficient one-pot methodology. The bioassay tests demonstrated that compounds 27 and 28 displayed much stronger antitumor activities against four human cancer cell lines (HepG2, A549, MDA-MB-231 and MCF-7) than positive control fluorouracil. Particularly, compound 28 showed a two-fold improvement compared to fluorouracil in inhibiting MDA-MB-231 and A549 cell proliferation with IC50 values of 7.46 and 12.78 μM, respectively. Further flow-activated cell sorting analysis revealed that the most promising compound 28 displayed a significant effect on G 2/M cell-cycle arrest in a dose-dependent manner in MDA-MB-231 cells.