本文選題：吲哚　切入點：二氨基嘧啶　出處：《有機化學》2017年04期 　論文類型：期刊論文

【摘要】：在課題組前期研究的基礎上,設計、合成了23個未見文獻報道的含吲哚結(jié)構(gòu)單元的2,4-二氨基嘧啶類化合物,其結(jié)構(gòu)經(jīng)~1H NMR,~(13)C NMR及HRMS確認.并采用噻唑藍(MTT)法測試了目標化合物對人子宮頸癌細胞(He La)、乳腺癌細胞(MD-MBA-231)、前列腺癌細胞(PC-3)、人結(jié)腸癌細胞(HCT116)的體外抗腫瘤活性.結(jié)果表明,大部分化合物具有一定的腫瘤抑制活性.尤其是2-[5-硝基-2-(6-氯-2-苯甲�；�-1H-吲哚-3-胺基)嘧啶-4-胺基]乙酸乙酯(8j)對HCT116、MD-MBA-231的體外腫瘤抑制活性比陽性對照藥品5-氟尿嘧啶分別高出2.0、0.5倍,體現(xiàn)出了較好的進一步研究價值.
[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.
【作者單位】： 南方醫(yī)科大學藥學院廣東省新藥篩選重點實驗室;
【基金】：國家自然科學基金(Nos.21102069、21372113) 廣州市珠江科技新星專項(No.2012J2200051)資助項目~~
【分類號】：O626;R914;R96
，

本文編號：1575088