香豆素苄(亚)砜类化合物的合成及其抗辐射活性评价  

Synthesis and anti-radiation activity of coumarinbenzyl(sulfoxide) sulfone derivatives

作　　者：周玉美[1,2,3] 唐林[2] 张首国[2] 彭涛[2] 王刚[2] 温晓雪[2] 刘曙晨[2] 孙云波[2] 王林[1,2] 

机构地区：[1]北京工业大学生命科学与生物工程学院,北京100124 [2]军事医学科学院放射与辐射医学研究所,北京100850 [3]中国医学科学院药物研究所,北京100050

出　　处：《国际药学研究杂志》2017年第5期427-431,460,共6页Journal of International Pharmaceutical Research

基　　金：国家自然科学基金资助项目(81273431)

摘　　要：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 Using Ex-Rad as lead compound to design and synthesize coumarin benzyl （sulfoxide） sulfone deriva- tives with anti-radiation activity. Methods The target compounds were synthesized from methyl 2-mercaptoacetate and 4-bromometh- ylbenzoic 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 struc- tures were confirmed by ^1H NMR and HRMS. Preliminary evaluation of the 16 compounds demonstrated that 6a, 6b, 6c and 6d exhibit- ed 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.

关 键 词：设计合成 香豆素 苄(亚)砜 抗辐射活性 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]