基于 1,4-二烷氧基萘的咪唑鎓盐的合成及其在癌细胞系中的细胞毒性。

Department of Applied Chemistry, Global Center for Pharmaceutical Ingredient Materials, Kyung Hee University, Yongin 1732, Republic of Korea.

Department of Gerontology, Graduate School of East-West Medicinal Science, Kyung Hee University, Yongin 17104, Republic of Korea.

Int J Mol Sci. 2023 Feb 1;24(3):2713. doi: 10.3390/ijms24032713.

In this study, we designed and synthesized novel 1,4-dialkoxynaphthalene-2-alkyl imidazolium salt (IMS) derivatives containing both 1,4-dialkoxynaphthalene and imidazole, which are well known as pharmacophores. The cytotoxicities of these newly synthesized IMS derivatives were investigated in order to explore the possibility of using them to develop anticancer drugs. It was found that some of the new IMS derivatives showed good cytotoxic activities. In addition, an initial, qualitative structure-activity relationship is presented on the basis of observations of activity changes corresponding to structural changes.

在这项研究中，我们设计并合成了新型的 1,4-二烷氧基萘-2-烷基咪唑啉盐（IMS）衍生物，其中含有 1,4-二烷氧基萘和咪唑啉，这两种结构均为药效团。为了探索将这些新合成的 IMS 衍生物用于开发抗癌药物的可能性，我们研究了它们的细胞毒性。结果发现，一些新的 IMS 衍生物具有良好的细胞毒性。此外，基于对结构变化引起的活性变化的观察，提出了初步的定性构效关系。