新型3-芳基香豆素类化合物的合成及其抗肿瘤活性

Synthesis and Antitumor Activities of Novel 3-Arylcoumarins

以芳基乙酸和取代邻羟基苯甲醛为起始原料,经Perkin缩合和关环反应合成了16个新型的3-芳基香豆素类化合物(3a^4h),其结构经1H NMR,IR和EI-MS表征。采用MTT法测定了3和4对人鼻咽癌细胞株(KB)、人气道平滑肌细胞株(KV)、人乳腺癌细胞株(MCF-7)、人乳腺癌多药耐药细胞株(MCF-7/ADR)的细胞毒性。结果表明:部分化合物表现出较强的细胞增殖抑制活性,其中7,8-二乙酰氧基-3-(4'-甲氧基苯基)香豆素(3e)对KB细胞的活性最强(IC505.88μmol·L-1)。

Sixteen novel 3-arylcoumarins（ 3a ～ 4h） were synthesized by Perkin reaction and cyclization reaction from aryl acetic acids and substituted 2-hydroxyl benzaldehydes. The structures were characterized by ^1H NMR,IR and EI-MS. The antitumor activities of 3a ～ 4h were investigated. The results showed that some compounds exhibited in vitro activities against human bobyrhinitis cancer（ KB）,human airway smooth muscle cancer（ KV）,human breast carcinoma（ MCF-7）,human breast carcinoma / multidrug resistance（ MCF-7 / ADR） cell lines to some extent. 7,8-Diacetoxy-3-（ 4＇methoxyphenyl） coumarin（ 3e） showed remarkable effect against KB tumor cells with IC50 of 5. 88 μmol·L^-1.