【摘要】 以苯甲醛或3,4-二甲氧基苯甲醛为原料经Wittig-Horner反应、Van Leusen吡咯合成法、水解等多步反应,设计并合成了16个未见文献报道的吡咯类氨基酸缀合物7a~7p.其结构经1H NMR,13C NMR及HRMS确证.采用噻唑蓝(MTT)法测试了目标化合物对MCF-7,MGC80-3,Hep G2,CT-26及HUVEC细胞的增殖抑制作用.结果表明,几乎所有化合物对人体正常细胞HUVEC无明显抑制作用,化合物7a~7h对Hep G2细胞株有一定的抑制活性,化合物7i~7p对MCF-7及MGC80-3较强的抑制活性.其中化合物7o~7p对MCF-7细胞株的抑制活性最强.更多还原

【Abstract】 Sixteen novel amino acid-conjugates of pyrrole derivatives 7a~7p were designed and synthesized using benzaldehyde or 3,4-dimethoxybenzaldehyde as raw materials. The compounds were synthesized via multi-step reaction including Wittig-Horner, Van Leusen and hydrolysis. The structures of all the target compounds were characterized by 1H NMR, 13 C NMR and HRMS. Moreover, the cell proliferation inhibiting activities of the target compounds were evaluated against MCF-7, MGC80-3, Hep G2, CT-26 and HUVEC cell lines by thiazolyl blue tetrazolium bromide(MTT) method. The result indicated that most of the compounds had no significant inhibitory effect against normal human cell HUVEC. However compounds 7a~7h showed significant inhibitory effect against Hep G2, compounds 7i~7p showed stronger inhibitory effect against MCF-7 and MGC 80-3, and compound 7o~7p exhibited the strongest inhibitory activity against MCF-7 in all of the compounds.更多还原