新型噻喃类似物对 MCF-7 乳腺癌和 HCT-15 结肠癌细胞的抗增殖活性：合成、细胞毒性、细胞周期分析和 DNA 结合。
Antiproliferative activity of novel thiopyran analogs on MCF-7 breast and HCT-15 colon cancer cells: synthesis, cytotoxicity, cell cycle analysis, and DNA-binding.
机构信息
Department of Chemistry, University of Canterbury, Christchurch, New Zealand.
出版信息
Nucleic Acid Ther. 2012 Aug;22(4):265-70. doi: 10.1089/nat.2012.0346. Epub 2012 Aug 16.
Abstract
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.
摘要
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。
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