Zhou Meiyun, Ji Shengbin, Wu Zhaojun, Li Yiqun, Zheng Wenjie, Zhou Hua, Chen Tianfeng
Department of Chemistry, Jinan University, Guangzhou 510632, PR China.
Department of Chemistry, Jinan University, Guangzhou 510632, PR China.
Eur J Med Chem. 2015;96:92-7. doi: 10.1016/j.ejmech.2015.03.069. Epub 2015 Apr 1.
A series of selenazolopyridine derivatives have been synthesized and characterized by X-ray diffraction, high resolution NMR and Mass spectrum. The in vitro anticancer activities of the synthetic compounds were screened against a panel of human cancer cell lines, human breast carcinoma MCF-7 cells, human liver carcinoma HepG2 cells and L02 normal cell line by MTT assay. By analyzing the structure-activity relationship among the synthetic compounds, it was found that 2-(phenylamino) selenazolo [5,4-b] pyridine, (PSeD, 7) had higher growth inhibitory effect on MCF-7 cells. The intracellular mechanism of cell death was evaluated by flow cytometric analysis and ROS assay, which revealed that PSeD could induce MCF-7 cells apoptosis by scavenging intracellular ROS. Taken together, we regard PSeD as an antioxidant which could inhibit cancer cell growth through induction of apoptosis.
一系列硒唑并吡啶衍生物已被合成，并通过X射线衍射、高分辨率核磁共振和质谱进行了表征。通过MTT法，针对一组人类癌细胞系，即人乳腺癌MCF-7细胞、人肝癌HepG2细胞和L02正常细胞系，筛选了合成化合物的体外抗癌活性。通过分析合成化合物之间的构效关系，发现2-(苯胺基)硒唑并[5,4-b]吡啶（PSeD，7）对MCF-7细胞具有更高的生长抑制作用。通过流式细胞术分析和活性氧检测评估了细胞死亡的细胞内机制，结果表明PSeD可通过清除细胞内活性氧诱导MCF-7细胞凋亡。综上所述，我们认为PSeD是一种抗氧化剂，可通过诱导凋亡抑制癌细胞生长。
