目的设计合成具有抗辐射活性的香豆素苄(亚)砜类衍生物。方法以Ex-Rad为先导化合物,设计香豆素苄(亚)砜类化合物16个;以2-巯基乙酸甲酯和4-溴甲基苯甲酸为起始原料,经3步反应合成目标化合物。通过抗辐射细胞实验测定目标化合物的抗辐射活性。结果合成16个未见文献报道的目标化合物,结构经~1H NMR和HRMS确证。初步药理结果显示,化合物6a、6b、6c和6d具有明显的抗辐射活性。结论目标化合物6a、6b、6c和6d具有显著的抗辐射活性,值得进一步研究。 Objective To design and synthesize coumarin benz (subscript) sulfone derivatives with antiradiation activity. Methods Ex-Rad as the lead compound was designed coumarin benzyl sulfone compounds 16; 2-mercaptoacetic acid methyl ester and 4-bromomethyl benzoic acid as the starting material, the synthesis of the target compound . The anti-radiation activity of the target compound was determined by anti-radiation cell experiments. Results Sixteen target compounds were synthesized and reported by ~ 1H NMR and HRMS. Preliminary pharmacological results show that compounds 6a, 6b, 6c and 6d have significant anti-radiation activity. Conclusion The target compounds 6a, 6b, 6c and 6d have significant anti-radiation activity, which deserves further study.