Synthesis of a new class of furo[3,2-c]coumarins and its anticancer activity

• A series of four furo[3,2-c]coumarin derivatives were synthesized.
• Antiproliferative activity against MCF-7 and HCT-15 cancer cell lines was evaluated.
• Two of the derivatives showed higher antiproliferative activity.
• UV/Vis spectroscopy was used for DNA and BSA-binding affinity.

A series of furo[3,2-c]coumarin derivatives 1a–d were synthesized and evaluated for their antiproliferative activity against MCF-7 breast and HCT-15 colon cancer cell lines using Sulfo-rhodamine B (SRB) assay. Compounds 1b and 1d showed higher antiproliferative activity than 1a and 1c. UV–Vis spectroscopy was used for DNA and BSA-binding affinity of the compounds 1b and 1d and gave overall affinity constants of K1b-DNA = 8.1 × 103 M−1, K1d-DNA = 1.1 × 104 M−1, K1b-BSA = 5.1 × 104 M−1, and K1d-BSA = 7.6 × 104 M−1. Our findings could provide new evidence showing the relationship between the chemical structure and anticancer activity of these new coumarin analogs.

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