论文部分内容阅读
以取代的苯乙酸为起始原料,通过成环、偶联、脱保护基并引入苯磺酰胺等反应得到了系列2,5-二取代-1,3,4-噻二唑类化合物,并利用1H NMR,13C NMR和HRMS对目标化合物进行了结构表征.用四甲基偶氮唑盐(MTT)法测试了目标化合物体外抑制前列腺癌细胞(PC-3)、乳腺癌细胞株(MDA-MB-231)和白血病细胞(K562)等肿瘤细胞的增殖活性.结果显示,部分目标化合物具有较好的抗肿瘤细胞增殖活性,其中(S)-N-(5-([1,1’-联苯]-4-基甲基)-1,3,4-噻二唑-2-基)-2-氨基-3-(4-溴苯基)丙酰胺(6a)和(S)-N-(5-([1,1’-联苯]-4-基甲基)-1,3,4-噻二唑-2-基)-2-氨基-3-苯基丙酰胺(6b)对K562细胞的活性与阳性对照药棉酚相当.
A series of 2,5-disubstituted-1,3,4-thiadiazoles were obtained from the substituted phenylacetic acids by ring-forming, coupling, deprotection and introduction of benzenesulfonamide. The target compounds were characterized by 1H NMR, 13C NMR and HRMS. The target compounds were tested for their ability to inhibit the proliferation of prostate cancer cells (PC-3), breast cancer cell lines (MDA- MB-231) and leukemia cells (K562). The results showed that some of the target compounds had good anti-tumor cell proliferative activity, among which, (S) -N- (5- Yl) -2,3-thiadiazol-2-yl) -2-amino-3- (4- bromophenyl) propanamide (6a) and (S) -N - (5 - ([1,1’-biphenyl] -4-ylmethyl) -1,3,4-thiadiazol- K562 cell activity and positive control gossypol equivalent.