Abstract
Cancer is one of the important health problems, and researchers continue their efforts to discover new anti-cancer agents. Coumarins (chromene-2-ones), a group of natural metabolites, have shown different biological activities based on their substitutions. In this study, 15 compounds of 1,5-dihydropyrano[2,3-c]chromene were synthesized by three-component reaction and investigated for the antiproliferative activity on the breast (MCF-7), colorectal (SW48 and HT-29), lung (A549), and brain (U-87 MG) cancer cell lines as well as two normal cell lines (3T3 and HUVEC). The apoptosis/necrosis-inducing effect of the selected compounds was determined on the MCF-7 cell line by flow cytometry. The results showed that the compounds bearing a moiety on their phenyl ring's para position had potent cytotoxic effects on the tested cell lines. These compounds induced apoptosis in MCF-7 cells. The compounds were also toxic for 3T3 and HUVECs and did not display a high selectivity for tumor cells. Our results revealed that the compounds having a moiety at the para position of their phenyl ring might be suitable lead compounds for the synthesis of potent anti-cancer agents.
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