Synthesis and Cytotoxic Activities of Novel Amino Acid-Conjugates of Pyrrole Derivatives

Sixteen novel amino acid-conjugates of pyrrole derivatives 7a~7p were designed and synthesized using benzal- dehyde 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 1 H 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 com-