Antiproliferative Activity of Novel Thiopyran Analogs on MCF-7 Breast and HCT-15 Colon Cancer Cells: Synthesis, Cytotoxicity, Cell Cycle Analysis, and DNA-Binding

摘要

A series of 6H-thiopyran-2,3-dicarboxylate derivatives 4a–d were synthesized and evaluated for their cytotoxic effect against HCT-15 colon and MCF-7 breast cancer cell lines using Sulforhodamine B (SRB) assay. The results showed that these compounds could exhibit a good cytotoxicity to both cell lines. In addition, these compounds were found to exhibit signi?cant DNA-binding af?nity. Ultraviolet–visible light (UV–Vis) spectroscopy was conducted to determine the ability of the ligand under analysis. The effect of ligand complexation on DNA structure led to overall af?nity constants of K4a = 3.5 · 10 4 M–1 , K4b = 6.4 · 10 4 M–1 , K4c = 3.2 · 10 4 M–1 , and K4d = 2.4 · 10 4 M–1 . Our ?ndings could provide new evidence showing the relationship between the chemical structure and biological activity and may be useful for the discovery of new anti-cancer drugs.