目的合成具有抗肿瘤活性的毛叶假鹰爪素C的B环衍生物。方法以2,4,6-三羟基苯乙酮为原料,经甲基化、O-甲基化、羟醛缩合3步反应制得目标产物,并以6个人肿瘤细胞株进行抗增殖活性评价。结果制备了14个目标化合物,其中9个为新化合物。经1H-NMR、13C-NMR,MS确证结构。结论初步活性研究表明,除1i的目标化合物均具有一定程度的抗肿瘤活性,1h和1n活性优于毛叶假鹰爪素C,B环引入两个F原子对化合物抗肿瘤活性具有一定贡献。 OBJECTIVE: To synthesize the B-ring derivatives of tacrolimus C with anti-tumor activity. Methods 2,4,6-trihydroxyacetophenone was used as raw material, and the target product was obtained by methylation, O-methylation and aldol condensation. The anti-proliferative activity of 6 human tumor cell lines was evaluated . Results 14 target compounds were prepared, of which 9 were new compounds. The structure was confirmed by1H-NMR, 13C-NMR, MS. CONCLUSION: The preliminary activity studies show that, except 1i, the target compounds have some antitumor activity, 1h and 1n activities are superior to the hairy chelonin C, and the introduction of two F atoms in the B ring contributes to the antitumor activity of the compounds.