1,3,4-恶二唑和1,2,4-三唑衍生物在癌细胞中的合成与抗增殖测定
Synthesis and antiproliferative assay of 1,3,4-oxadiazole and 1,2,4-triazole derivatives in cancer cells.
作者信息
Tu Guogang, Yan Yugang, Chen Xueying, Lv Qiaoli, Wang Jiaqi, Li Shaohua
机构信息
Department of Medicinal Chemistry, School of Pharmacy, Nanchang University, Nanchang, Jiangxi, China.
出版信息
Drug Discov Ther. 2013 Apr;7(2):58-65.
A series of new 1,3,4-oxadiazole and 1,2,4-triazole derivatives were synthesized. The structures were confirmed by IR, (1)H-NMR, and MS. The compounds were evaluated for their antiproliferative activity against K562 (human erythromyeloblastoid leukemia cell line), MDA-MB-231 (human breast adenocarcinoma cell line), HT29 (human colon adenocarcinoma grade II cell line) and HepG2 (human hepatocellular liver carcinoma cell line) in vitro. The result showed that 7 compounds displayed inhibitory activities against K562 with the inhibition rate more than 50%. Especially, compound 5f exhibited the most potent activity against K562 with 85% inhibition ratio and could be used as lead compound to search new 1,3,4-oxadiazole derivatives as antiproliferative agent.
合成了一系列新型的1,3,4-恶二唑和1,2,4-三唑衍生物。通过红外光谱、¹H-核磁共振和质谱对其结构进行了确证。对这些化合物在体外针对K562（人红白血病细胞系）、MDA-MB-231（人乳腺腺癌细胞系）、HT29（人结肠腺癌二级细胞系）和HepG2（人肝癌细胞系）的抗增殖活性进行了评估。结果表明，有7种化合物对K562表现出抑制活性，抑制率超过50%。特别是，化合物5f对K562表现出最有效的活性，抑制率为85%，可作为先导化合物来寻找新型的1,3,4-恶二唑衍生物作为抗增殖剂。
Zotero 插件