Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.

@article{Diao2017SynthesisAB,
  title={Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.},
  author={Peng-Cheng Diao and Qiu Li and Meng-Jin Hu and Yu-feng Ma and Wen-wei You and Kwon Ho Hong and Pei-liang Zhao},
  journal={European journal of medicinal chemistry},
  year={2017},
  volume={134},
  pages={110-118}
}
Based on our previous screening hit compound 1, a series of novel indole-pyrimidine hybrids possessing morpholine or thiomorpholine moiety were synthesized via an efficient one-pot multistep synthetic method. The antiproliferative activities of the synthesized compounds were evaluated in vitro against four cancer cell lines including HeLa, MDA-MB-231, MCF-7, and HCT116. The results revealed that most compounds possessed moderate to excellent potency. The IC50 values of the most promising… CONTINUE READING