Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (1): 167-174.DOI: 10.6023/cjoc201407016 Previous Articles     Next Articles



李衍忠, 赵萍, 詹晓平, 刘增路, 毛振民   

  1. 上海交通大学药学院 上海 200240
  • 收稿日期:2014-07-10 修回日期:2014-08-20 发布日期:2014-09-12
  • 通讯作者: 毛振民
  • 基金资助:

    国家“重大新药创制”科技重大专项(No. 2010ZX09401404-004)资助项目.

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

Li Yanzhong, Zhao Ping, Zhan Xiaoping, Liu Zenglu, Mao Zhenmin   

  1. School of Pharmacy, Shanghai Jiaotong University, Shanghai 200240
  • Received:2014-07-10 Revised:2014-08-20 Published:2014-09-12
  • Supported by:

    Project supported by the National Science and Technology Major Special Drug Discovery (No. 2010ZX09401404-004).

Sixteen novel amino acid-conjugates of pyrrole derivatives 7a7p 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, 13C 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 7a7h showed significant inhibitory effect against Hep G2, compounds 7i7p showed stronger inhibitory effect against MCF-7 and MGC 80-3, and compound 7o7p exhibited the strongest inhibitory activity against MCF-7 in all of the compounds.

Key words: pyrrole, amino acid, synthesis, cytotoxic activities