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以(R)-2-(4-羟基苯氧基)丙酸和氯代吡啶为起始原料,设计并合成了系列N-吡啶基-2-(4-芳氧苯氧基)丙酰胺化合物,其结构经1HNMR、LC-MS、13CNMR、IR和元素分析证实,对化合物立体构型与反应条件的关系进行了研究。采用MTT法测定了其对A549和Hela细胞系的活性,结果表明,所合成化合物具有不同程度的抗肿瘤活性,其中N-(3-硝基吡啶-2-基)-2-[4-[(6-氯喹喔啉-2-基)氧基]苯氧基]丙酰胺(Ⅳf)(IC50=0.007 mmol/L)比顺铂(IC50=0.026 mmol/L)抗肿瘤活性高。
A series of N-pyridyl-2- (4-aryloxyphenoxy) propanamide compounds were designed and synthesized using (R) -2- (4-hydroxyphenoxy) propionic acid and chloropyridine as starting materials Its structure was confirmed by 1HNMR, LC-MS, 13CNMR, IR and elemental analysis. The relationship between the stereoconfiguration and reaction conditions was studied. MTT assay was used to determine the activity of A549 and Hela cell lines. The results showed that the compounds have different antitumor activities. Among them, N- (3-nitropyridin-2-yl) -2- [4- [ (IVf) (IC50 = 0.007 mmol / L) showed higher anti-tumor activity than cisplatin (IC50 = 0.026 mmol / L)