黄芩素氨基酸衍生物的合成及体外细胞毒活性评价（英文）

目的：合成天然产物黄芩素的氨基酸衍生物并进行体外抗肿瘤活性评价。方法：氨基酸经酯化和酰化,在吡啶溶液中通过甲醛与黄芩素反应,制得黄芩素8位引入氨基酸侧链的衍生物;氨基酸经羧基保护和氨基酰化、黄芩素经羟基保护,制得黄芩素6位引入氨基酸侧链的衍生物。衍生物结构经质谱（MS）、核磁共振光谱（NMR）和红外光谱（IR）确证。结果：设计合成了未见文献报道的13个新的黄芩素衍生物,采用MTT法评价了目标化合物对人肝癌细胞HepG2生长的抑制活性。结论：化合物4c,4d,7a和7b显示较黄芩素高的体外抗肿瘤活性。

Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

AIM： To synthesize the baicalein amino acid derivatives and evaluate their cytotoxicity activities in vitro. METHODS： Amino acids were subjected to methylation and aminoacylation reaction, then reacted with formaldehyde and baicalein to synthesize baicalein-8 benzyl amino acid derivatives. Through carboxyl group protection and aminoacylation of amino acid and benzyl protection of baicalein, derivatives of baicalein-6-O-amino acid esters were obtained. All of the target compounds were identified by IR, MS and ~H NMR. RESULTS： Thirteen novel derivatives were synthesized and characterized. Their cytotoxic activities were assessed by the MTT method on the inhibition of HepG2 cells in vitro. CONCLUSION： Compounds 4c, 4d, 7a and 7b showed a significant increase in cytotoxicity compared with baicalein.