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 significant DNA-binding affinity. 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 affinity constants of K
4a
= 3.5 · 10
4
M
–1
, K
4b
= 6.4 · 10
4
M
–1
, K
, and
K
4d
= 2.4 · 10
4
M
–1
. Our findings 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.
کلید واژگان :
Antiproliferative Activity, Colon Cancer Cells, DNA-Binding
