军事医学2024，Vol.48Issue(1)：20-29,10.DOI:10.7644/j.issn.1674-9960.2024.01.005
取代2H-苯并吡喃-3-甲酰苯胺化合物的合成及抗辐射活性评价
Synthesis and anti-radiation activity evaluation of substituted 2H-benzopyran-3-formylaniline compounds
摘要
Abstract
Objective To discover new-structure active molecules in order to provide candidate compounds for anti-radiation drug research.Methods Conformational fixation and functional group conversion strategies were used to modify the structure of Ex-RAD before substituted 2H-benzopyran-3-formylaniline compounds were designed and synthesized.The anti-radiation activities of the synthesized compounds were screened via irradiated cell survival models and the cytotoxicity of the active compounds was examined.Western blotting assay was used to investigate the effects of the optimal compound on the expressions of apoptosis related proteins in irradiated cells.The anti-radiation activity of the optimal compound was evaluated through irradiated mice models.Results Twenty-one target compounds were synthesized,eight of which were found to significantly improve the survival of irradiated cells.Four compounds were selected for re-screening and cytotoxicity evaluation.Compound D19 was determined as the optimal compound that could affect the expressions of apoptosis related proteins in irradiated AHH-1 cells by Western blotting assay.Compared with the radiation group,the 30-day survival rate of D19 treated mice irradiated with 8.6 Gy of whole-body radiation increased by 70%.D19 showed protective effect on the blood system of non-lethal dose irradiated mice.Conclusion The novel compound D19 has shown strong anti-radiation activity and deserves more research.关键词
苯并吡喃/化合物合成/抗辐射/评价Key words
benzopyran/compound synthesis/anti-radiation/evaluation分类
医药卫生引用本文复制引用
彭涛,李旭平,徐菁,张首国,王林..取代2H-苯并吡喃-3-甲酰苯胺化合物的合成及抗辐射活性评价[J].军事医学,2024,48(1):20-29,10.基金项目
军队医学科技青年培育计划(21QNPY149) （21QNPY149）
