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.
Volume 133, 2021
Continuous Article Publishing mode
Click here for Editorial Note on CAP Mode