A series of1,2,4- and 1,3,4-oxadiazole derivatives were synthesized and evaluated for their anticancer activity. Halogenated 1,2,4-oxadiazoles were obtained from benzonitrile and coupled either lipophilic amines or with aminoalcohols. Lipophilic 1,3,4-oxadiazole derivatives were obtained through the Mannich reactions between 5-(aryl)-1,3,4-oxadiazole-2-thiol and alkylated or acylated amines. The in vitro
合成了一系列1,2,4-和1,3,4-恶二唑衍
生物,并评估了其抗癌活性。卤代的
1,2,4-恶二唑从
苄腈获得,并与亲脂性胺或
氨基醇偶联。亲脂性1,3,4-恶二唑衍
生物是通过5-(芳基)-1,3,4-恶二唑-2-
硫醇与烷基化或酰化胺之间的曼尼希反应获得的。在体外的细胞毒性效应对4T1-乳腺癌评价和CT26 -结肠癌细胞。1,3,4-恶二唑与具有10-14个碳链部分的烷基化
哌嗪偶联的IC 50为最佳 对于4T1
细胞系,其值范围为1.6至3.55μM,对于CT26.WT
细胞系,其值范围为1.6至3.9μM,选择性指数最高为19。最有效的化合物采用AnnexinV和
PI染色进行了研究,可作为细胞凋亡诱导的指示。