7-甲氧基黄酮及衍生物的合成与体外抗乳腺癌细胞活性

Synthesis and in vitro Anti-breast Cancer Activity of 7- Methoxy Flavone and its Derivatives

本文对7-甲氧基黄酮及其衍生物的合成与抗乳腺癌细胞的活性进行了研究。以邻、对位酚羟基苯乙酮为起始原料,利用硫酸二甲酯对其部分酚羟基进行甲基化生成邻羟基甲醚类苯乙酮。得到的产物与苯甲醛及其衍生物发生羟醛缩合反应生成2-羟基查尔酮及其衍生物。通过经典的AFO反应和强碱条件下分子内加成反应分别生成了黄酮醇、黄酮及衍生物。同时,采用MTT法研究了目标化合物体外抑制乳腺癌MDA-231细胞的活性。芳香化合物2、7、10表现明显的体外抗乳腺癌细胞活性。因此,7-甲氧基黄酮及衍生物很有可能成为新型结构的抗癌先导化合物。

The synthesis and anti-breast cancer activity of 7-methoxy flavone and its derivatives were studied. Selective methylatiun of ortho- and para- phenol hydroxyl acetophenune with dlmethylsulfate, delivered corresponding acetophenune products. The resulting products reacted with benzaldehyde to give 2-hydroxy! chalcone and its derivatives. Following AFO reaction and intramolecular addition reaction under basic conditions, flavonols, flavonoids and its derivatives were synthesized. Furthermore ,the in vitro antitumor activity of novel synthesized compounds to breast cancer cell line MDA- 231 was evaluated by MTT assay. Results indietacd that aromatic compounds 2,7 and 10 showed potential antitumor ac- tivity. Therefore ,7-methoxy flavone and its derivatives can be promising antitumor lead compounds.