N-芳乙基异喹啉衍生物的合成及其抗肿瘤活性研究

Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents

摘要:
本研究采用一种简便的新方法设计合成了一系列全新结构的N-芳乙基异喹啉衍生物, 并对其体外抗肿瘤活性进行了评价。其中化合物9a表现出较强的抗肿瘤活性, 对人肝癌HepG2和大肠癌HCT116细胞的IC₅₀值分别为2.52和1.99 μg·mL^–1。初步作用机制显示, 9a可以将HepG2细胞周期阻滞于S期, 使细胞增殖受阻, 达到抗肿瘤效果。

Abstract:
A series of novel N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities. Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC₅₀values of 2.52 and 1.99 μg·mL^–1, respectively. Cell cycle was blocked at S phase of HepG2 cells treated with 9a by flow cytometry detection. Our results provided a basis for the development of a new series of anti-cancer candidates.