Evaluation of the Cytotoxic Effect and Antiproliferative Activity of 3-Carboxylated Coumarins Derivatives in an In Vitro Model

ABSTRACTHerein we report an exploratory study based on the cytotoxicity and antiproliferative activity of four previously synthesized coumarins derivatives (compounds 1a-d). The cytotoxic effect of the compounds was assessed on mononuclear cells, which were obtained from blood samples of healthy donors and measured by XTT method. The antiproliferative activity experiments were developed using HeLa, CaSKi and SiHa cervical cancer cell lines, and was evaluated by the MTT assay. In every single experiment, Cisplatin as internal control was employed. The cytotoxic assessment revealed that the four compounds did not significantly affect the viability on normal cells, whereas the antiproliferative activity on cancer cells was variable, according to the substituent located at position 3 of the coumarin core. It is worth mentioning that compound 1c, compared with the other products, presented a remarkable effect against CaSKi cell line, likewise 1d but in HeLa cells. These findings suggest that there is a relationship between biological activity and the alkoxycarbonyl chain since this is the only structural difference among the four tested compounds. The results lead to conclude that butyl group which is the substituent in compound 1d, was the key element in the antiproliferative effect presented by the molecule against SiHa, CaSKi and HeLa cell lines. Keywords: Coumarins, Tumor cells, Mononuclear cells, Cis-Platin, Cytotoxicity, MTT.