Synthesis and Antiproliferative Effect of Novel Curcumin Analogues

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  • Liu Bingmi
    Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University College of Pharmacy, Liaoning University
  • Xia Mingyu
    School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
  • Ji Xiaoling
    School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
  • Xu Liying
    Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University
  • Dong Jinhua
    Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University

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Novel curcumin analogues with α,β-unsaturated ketone moiety and/or α,β-saturated ketone structure were synthesized from curcumin via alkylation at the central carbon and the phenolic hydroxy groups, and hydrogenation of α,β-unsaturated ketone moiety. The antiproliferative activities were tested in five human solid tumor cell lines in vitro. Most of the compounds exhibited increased antiproliferative activities comparing with that of curcumin. Structure–activity relationship (SAR) analysis revealed that the α,β-unsaturated ketone structure was not required for antiproliferative activity of these curcumin analogues. Among these compounds, 1,7-bis(3-methoxy-4-(3-(4-methylpiperazinyl-1-yl)propoxy)phenyl)-4,4-dibenzylheptane-3,5-dione (16f) was the most effective one with IC50 value below 1 µM, which was 9- to 81-fold more potent than curcumin.

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