含吲哚环2,4-二氨基嘧啶类化合物的合成及抗肿瘤活性

发布时间：2018-03-06 13:49

  本文选题：吲哚　切入点：二氨基嘧啶　出处：《有机化学》2017年04期 　论文类型：期刊论文

【摘要】：在课题组前期研究的基础上,设计、合成了23个未见文献报道的含吲哚结构单元的2,4-二氨基嘧啶类化合物,其结构经~1H NMR,~(13)C NMR及HRMS确认.并采用噻唑蓝(MTT)法测试了目标化合物对人子宫颈癌细胞(He La)、乳腺癌细胞(MD-MBA-231)、前列腺癌细胞(PC-3)、人结肠癌细胞(HCT116)的体外抗肿瘤活性.结果表明,大部分化合物具有一定的肿瘤抑制活性.尤其是2-[5-硝基-2-(6-氯-2-苯甲酰基-1H-吲哚-3-胺基)嘧啶-4-胺基]乙酸乙酯(8j)对HCT116、MD-MBA-231的体外肿瘤抑制活性比阳性对照药品5-氟尿嘧啶分别高出2.0、0.5倍,体现出了较好的进一步研究价值.
[Abstract]:On the basis of the previous study of the research group, 23 2O4-diaminopyrimidine compounds containing indole-containing structural units were designed and synthesized. Its structure was confirmed by 1H NMR-13C NMR and HRMS. The in vitro antitumor activity of the target compound against human cervical cancer cell line he Lahmen, breast cancer cell line MD-MBA-231, prostate cancer cell line PC-3H, human colon cancer cell line HCT116) in vitro was determined by using thiazolyl methacrylate method. Most of the compounds have a certain tumor inhibitory activity, especially 2- [5- [5-nitro-2-butadiene-6-chloro-2-benzoyl] pyrimidine -4-aminoethyl ester 8j) on HCT116MD-MBA-231, which is more effective than 5-fluorouracil in vitro in inhibiting HCT116MD-MBA-231. Pyrimidine was 0.5 times higher than 2. 0%, respectively. It reflects the value of further research.
【作者单位】： 南方医科大学药学院广东省新药筛选重点实验室;
【基金】：国家自然科学基金(Nos.21102069、21372113) 广州市珠江科技新星专项(No.2012J2200051)资助项目~~
【分类号】：O626;R914;R96
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本文编号：1575088