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    • Keywords


      Anti-proliferative activity; Cancer; Coumarin; Hydrazide–hydrazone; Molecular hybridization

    • Abstract


      A series of 21 coumarin hydrazide–hydrazone derivatives were designed, synthesized and evaluated potential cytotoxicity effects at 25 lg/mL for 48 h against liver cancer (HepG2) cell line in vitro. Then, seven out of 21 compounds with % cell viability lower than 60% were selected for evaluation of in vitro anti-proliferative activity against liver cancer (HepG2), breast cancer (SKBR-3) and human colon cancer (Caco-2) cell lines. Among the test compounds, 5g, 6d and 6f showed potent activities against both Hep-G2 and SKBR-3 cell lines. More significantly, compound 6d, having a 4-bromophenyl moiety, exhibited best cytotoxic activity against Hep-G2 cell line with IC50 value of 2.84 ± 0.48 lg/mL which is comparable to the standard doxorubicin (IC50 = 2.11 ± 0.13 lg/mL). In addition, compound 6f, having 4-methoxyphenyl moiety, demonstrated the most potent activity (IC50 = 2.34 ± 0.68 lg/mL) against SKBR-3 cell line oncomparison with other tested coumarin hydrazide–hydrazone derivatives. Unfortunately, all test compounds, as well as doxorubicin, showed no cytotoxicity toward drug-resistant cell line, Caco-2. Our preliminary results indicated that coumarin hydrazide–hydrazone derivatives could be exploited as leading structures for further anticancer-drug development.

    • Author Affiliations



      1. Drug Discovery and Development Center, Office of Advanced Science and Technology, Thammasat University, Pathumthani 12121, Thailand
      2. Department of Chemistry, Faculty of Science and Technology, Thammasat University, Pathumthani 12121, Thailand
    • Dates

  • Journal of Chemical Sciences | News

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      Posted on July 25, 2019

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