Department of Chemistry, University of Canterbury, Christchurch, New Zealand.
Nucleic Acid Ther. 2012 Aug;22(4):265-70. doi: 10.1089/nat.2012.0346. Epub 2012 Aug 16.
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(4c)=3.2×10(4) M(-1), 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.
一系列 6H-噻喃-2,3-二羧酸酯衍生物 4a-d 被合成，并通过磺基罗丹明 B（SRB）试验评估它们对 HCT-15 结肠和 MCF-7 乳腺癌细胞系的细胞毒性。结果表明，这些化合物对两种细胞系均表现出良好的细胞毒性。此外，这些化合物被发现具有显著的 DNA 结合亲和力。紫外-可见光谱（UV-Vis）用于确定分析配体的能力。配体络合对 DNA 结构的影响导致整体结合常数 K(4a)=3.5×10(4) M(-1)、K(4b)=6.4×10(4) M(-1)、K(4c)=3.2×10(4) M(-1)和 K(4d)=2.4×10(4) M(-1)。我们的研究结果可以提供新的证据，表明化学结构与生物活性之间的关系，可能有助于发现新的抗癌药物。
