Synthesis and anti-radiation activity of coumarinbenzyl (sulfoxide) sulfone derivatives / 国际药学研究杂志

ABSTRACT

Objective Using Ex-Rad as lead compound to design and synthesize coumarin benzyl(sulfoxide)sulfone derivatives with anti-radiation activity. Methods The target compounds were synthesized from methyl 2-mercaptoacetate and 4-bromomethylbenzoic acid through three steps. The anti-radiation activity was assayed by the MTT method using the HUVEC cells irradiated with 8Gy 60Co γ ray. Results Sixteen compounds containing a coumarin benzyl sulfoxide or sulfone group were synthesized and the structures were confirmed by 1H NMR and HRMS. Preliminary evaluation of the 16 compounds demonstrated that 6a, 6b, 6c and 6d exhibited potent anti-radiation activities. Conclusion The anti-radiation activities of 6a, 6b, 6c and 6d were significant, indicating that this kind of compounds is worth further study.