白杨素衍生物的合成及其抗肿瘤活性

利用Baker-Venkataraman重排法，以2,4,6-三羟基苯乙酮为原料，经羟基保护、酰化、重排、成环、脱保护5步反应全合成白杨素。以白杨素为骨架，再利用7位羟基的活性，在C-7位引入水溶性基团——烷胺基，设计合成了未见文献报道的21种白杨素系列衍生物8a-8u，其结构经¹H NMR、¹³C NMR、IR和MS确证。采用MTT法评价了目标化合物对HCT-116(人体结肠癌细胞系)，HeLa（人体宫颈癌细胞系），DU-145（人体前列腺癌细胞系），SGC-7901(人体胃癌细胞系)和HEK-293(人胚肾细胞系)的抗肿瘤活性。其体外抗肿瘤活性实验表明，7-(2-哌嗪乙氧基)-5-羟基-2-苯基-4H-1-苯并吡喃-4-酮(8o)具有较好的抗肿瘤活性。

Synthesis and antitumor activity of novel chrysin derivatives

Chrysin was synthesized in five steps starting from 2,4,6-trihydroxyacetophenone via methylation,acylation,Baker-Venkataraman rearrangement,cyclization and deprotection.With chrysin as the lead compound,novel chrysin derivatives 8a-8u were designed and synthesized.The chemical structures of these compounds were confirmed by 1H NMR,13C NMR,IR and MS.Twenty-one new chrysin derivatives were prepared and their antitumor activities were evaluated by MTT method on HCT-116(human colon cancer cell line),HeLa(human ...