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以4-雄烯二酮1为原料,用金催化甾炔法设计并合成了一系列17-(2′,5′-二取代噁唑基)-雄甾-4,16-二烯-3-酮衍生物4a~4k.所合成产物通过1H NMR,13C NMR,IR和HRMS方法进行了结构表征.以阿比特龙为阳性对照,通过3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)法测试了目标化合物对MCF-7(人乳腺癌细胞)、A549(人肺癌细胞)、Bel-7402(人肝癌细胞)、Hela(人宫颈癌细胞)和PC-3M-1E8(人前列腺癌细胞)的体外抗肿瘤活性.结果表明大多数化合物表现出了较好的抗肿瘤活性,其中化合物4c,4g,4i和4j的抗肿瘤活性与阳性对照物阿比特龙相当,且所测化合物对MCF-7有较好选择性作用,其IC50值在3.0~25.5μmol/L之间.
A series of 17- (2 ’, 5’-disubstituted oxazolyl) -androsta-4,16-diene-3 were synthesized using 4-androstenedione 1 as raw materials. -ketone derivatives 4a ~ 4k.The synthesized products were characterized by 1H NMR, 13C NMR, IR and HRMS methods.Arabidon was used as a positive control, and 3- (4,5-dimethylthiazol-2-yl) (Human breast cancer cell line), A549 (human lung cancer cell line), Bel-7402 (human liver cancer cell line), Hela (human liver cancer cell line) Human cervical cancer cells) and PC-3M-1E8 (human prostate cancer cells) in vitro.Results showed that most of the compounds showed good anti-tumor activity, and anti-tumor of compounds 4c, 4g, 4i and 4j The activity was comparable to the positive control Abiraterone, and the compounds tested showed good selectivity for MCF-7 with IC50 values of 3.0-25.5 μmol / L.