Synthesis and Anti-hepatoma Activities of N-(Piperidin-4-yl)benzamide Derivatives

doi:10.11944/j.issn.1000-0518.2016.06.150358

Chinese Journal of Applied Chemistry ›› 2016, Vol. 33 ›› Issue (6): 661-667.DOI: 10.11944/j.issn.1000-0518.2016.06.150358

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Synthesis and Anti-hepatoma Activities of N-(Piperidin-4-yl)benzamide Derivatives

HUANG Zhining^a,ZHENG Manyi^a,MIAO Fangxiao^b,YU Jingqi^a,LI Shanhua^b,LI Funan^a,QU Ning^b^*()

^a School of Pharmaceutical Sciences,Xiamen University,Xiamen,Fujian 361102,China
^b Medical College,Xiamen University,Xiamen,Fujian 361102,China

Received:2015-10-10 Accepted:2016-02-18 Published:2016-06-01 Online:2016-06-01
Contact: QU Ning
Supported by:
Supported by the Natural Science Foundation of Fujian Province of China(No.2015Y0081), XMU Training Program of Innovation and Enterpreneurship for Undergraduates(No.201510384055;No.20720152005)

Abstract

Abstract:

Six benzamide derivatives were synthesized from 4-hydroxybenzoic acid via alkylation, hydrolysis and condensation reactions. The structure was confirmed by ¹H NMR, ¹³C NMR and MS. The antitumor activity of all the newly synthesized compounds was evaluated on the in vitro growth of HepG2 cell line using sorafeinb as positive control. The anti-hepatoma biological activity in vitro of N-(1-(methylsulfonyl)piperidin-4-yl)-4-phenoxybenzamide is better than that of sorafeinb with an IC₅₀ value of 8.42 μmol/L. The results show that the derivatives of N-(piperidin-4-yl)-4-phenoxybenzamide have good anti-hepatoma activity.

Key words: benzamide, HepG2 cells, anti-hepatoma activity

HUANG Zhining, ZHENG Manyi, MIAO Fangxiao, YU Jingqi, LI Shanhua, LI Funan, QU Ning. Synthesis and Anti-hepatoma Activities of N-(Piperidin-4-yl)benzamide Derivatives[J]. Chinese Journal of Applied Chemistry, 2016, 33(6): 661-667.

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Synthesis and Anti-hepatoma Activities of N-(Piperidin-4-yl)benzamide Derivatives

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