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以3-甲基-2-氰基吡啶为原料,经水解、酯化、硝化、甲氧基取代、溴代反应制得中间体3-溴甲基-5-甲氧基吡啶-2-甲酸甲酯(7),然后中间体与不同的有机胺经环合反应得到一系列新的沙利度胺衍生物3-甲氧基-6-取代-5,6-二氢吡咯[3,4-b]吡啶-7-酮1a~1l.其结构经1H NMR,13C NMR及HRMS确证.采用MTT(噻唑蓝)法测试了目标化合物抑制HCT-116,MG-63,MCF-7,HUVEC及HMVEC细胞的活性,结果表明,几乎所有化合物对人体正常细胞无明显抑制作用,化合物1h~1l只对MG-63细胞株有明显的抑制活性,化合物1c~1g对这三种肿瘤细胞都有较强的抑制活性,其中化合物1d和1e活性最强.
3-Methyl-2-cyanopyridine was used as starting material to prepare 3-bromomethyl-5-methoxypyridine-2-carboxylic acid through hydrolysis, esterification, nitration, methoxy substitution and bromination Methyl ester (7), and then intermediates with different organic amines by cyclization to give a series of new thalidomide derivatives 3-methoxy-6-substituted-5,6-dihydropyrrolo [3,4 1H-NMR, 13C NMR and HRMS were used to confirm the inhibitory effect of the target compound on HCT-116, MG-63, MCF-7, HUVEC and HMVEC cell activity, the results showed that almost all compounds on human normal cells had no significant inhibitory effect of compounds 1h ~ 1l only MG-63 cell lines had significant inhibitory activity of compounds 1c ~ 1g of these three tumor cells are more Strong inhibitory activity, of which compounds 1d and 1e were the most active.