Synthesis and antitumor activity of 13-acylmatrine derivatives
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维普
目的：合成13-酰胺基取代苦参碱衍生物及研究该类化合物的体外抗肿瘤活性。方法以槐果碱为原料，通过迈克尔加成（Michael addition），叠氮还原酰化反应，制得系列13-位酰胺取代的衍生物，所有化合物结构均经1 H NMR等谱确证；选取人肝癌细胞（BEL-7404）和小鼠黑色素瘤细胞（K111）对所合成的目标化合物进行体外抗肿瘤药理活性筛选。结果设计合成了9个新化合物，大多数化合物对两株肿瘤细胞都具有较强的抑制活性。结论化合物4b和4e对人肝癌细胞（BEL-7404）有较强的抑制活性。
Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity . Methods Using sophocarpine as the starting material ,a series of new compounds were synthesized through Michael addition , Staudinger reduction and acylation .The structure of target compounds were confirmed by 1 H NMR and MS techniques .Their antitumoractivityagainsthumanhepatomacells(BEL-7404)andmicemelanomacells(K111)wereevaluated invitrobyMTT assay .Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111 . Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404) .
NETL
NSTL
万方数据
维普
