Design, Synthesis, and Anti-Breast Cancer Activity of Some Hybrid Molecules Containing Coumarin Moiety

(Benzimidazol-2-yl)-7-hydroxycoumarin and N-(2-hydroxyphenyl)-7-hydroxycoumarin-3-carboxamide have been synthesized by the condensation of ethyl 7-hydroxycoumarin-3-carboxylate in acetic acid. Acetylation with acetic anhydride and halogenation with bromine in acetic acid's presence of the previous compounds has yielded the corresponding acetoxy and dibromo derivatives. The synthesized molecules that contain coumarin ring have been evaluated for their activities against breast cancer and they have shown good in vitro antiproliferative activities against a human breast cancer line (MCF-7). The results have shown that 3-(benzimidazol-2-yl)-7-acetoxycoumarin had a significant cytotoxic effect compared to the standard DOX (doxorubicin) drug.

Automated summary

Benzimidazol-2-yl)-7-hydroxycoumarin and N-(2-hydroxyphenyl)-7-hydroxycoumarin-3-carboxamide were synthesized through condensation in acetic acid, followed by acetylation and halogenation. The synthesized molecules showed good in vitro antiproliferative activities against breast cancer, particularly 3-(benzimidazol-2-yl)-7-acetoxycoumarin which exhibited a significant cytotoxic effect compared to the standard drug DOX (doxorubicin).