Synthesis of new imine-/amine-bearing imidazo[1,2-a]pyrimidine derivatives and screening of their cytotoxic activity

Imidazo[1,2- ]pyrimidine derivatives bearing imine groups ( - ) were successfully synthesized in moderate to good yields using microwave-assisted heating. Corresponding amine derivatives ( - ) were also obtained by the reduction reaction of the imine derivatives ( - ). All synthesized products were characterized by FT-IR, H NMR, C NMR, and LC-MS spectroscopic techniques. In silico ADMET, Lipinski, and drug-likeness studies of the compounds were conducted and all were found to be suitable drug candidates. The cytotoxicity of the potential drug molecules was screened against the breast cancer cell lines MCF-7 and MDA-MB-231 and the healthy model HUVEC by the sulforhodamine B method. According to the antiproliferative studies, compounds and showed remarkable inhibition of MCF-7 cells with IC values of 43.4 and 39.0 μM and of MDA-MB-231 cells with IC values of 35.9 and 35.1 μM, respectively. In particular, compound selectively inhibited the proliferation of MCF-7 1.6-fold and MDA-MB-231 2.0-fold relative to healthy cells. Moreover, the apoptotic mechanism studies indicated that compound induced apoptosis by moderately increasing the ratio of Bax/Bcl-2 genes. Imidazo[1,2- ]pyrimidine derivative , a promising cytotoxic agent, may be helpful in the discovery of new and more efficient anticancer agents for breast cancer treatment.