C-13位烷氧基赤霉素衍生物的合成与抗肿瘤活性研究

Synthesis and Anticancer Activities of C-13 Etheral Gibberellin Derivatives

设计并合成了系列C-13位为醚结构且在A环和D环有两个α,β-不饱和酮结构的赤霉素衍生物.采用噻唑蓝(MTT)法评价了其对人肺腺癌细胞(A549)、人肝癌细胞(HepG2)、人胃癌细胞(MKN28)以及结肠癌细胞(HT29)的体外生长抑制作用,结果表明:此类化合物都有较强的体外抗肿瘤活性,其中化合物27的活性最强(对人胃癌细胞MKN28的IC50=0.21μmol·L-1),优于阳性对照药物顺铂(DDP).

C-13 ethereal gibberellin derivatives bearing two α,β-unsaturated ketones in A and D rings have been designed and synthesized. In vitro studies demonstrated that a number of the C-13 ethereal gibberellin derivatives showed strong anticancer activities in thiazolylblue （MTT） assay towards four human cancer cell lines including HT29, A-549, HepG2 and MKN28. Compound 27 was found to be the most potent compound （IC50=0.21 μmol L-1 against MKN28） and more active than the positive control （DDP）.