Dipartimento di Scienze del Farmaco, Università di Catania, Viale Andrea Doria 6, Catania 95125, Italy.
Bioorg Med Chem. 2012 Aug 15;20(16):4978-84. doi: 10.1016/j.bmc.2012.06.035. Epub 2012 Jun 26.
This paper reports the synthesis and the biological properties of two novel pyrene-bearing isoxazolidinyl derivatives able to exhibit antitumor activity by DNA intercalation. The synthetic approach exploits a consolidated protocol based on 1,3-dipolar cycloaddition reaction. The intercalating properties have been determined by combining electrophoresis studies with molecular docking, while the antitumor activity has been evaluated over five carcinoma cell lines. The obtained compounds show also a good affinity towards silver cations; the presence of a 2-hydroxybenzyl appendage on the isoxazolidine ring ensures a good affinity and selectivity in the binding.
本文报道了两种新型含芘的异恶唑啉衍生物的合成及生物学性质，它们能够通过 DNA 嵌入发挥抗肿瘤活性。该合成方法利用了基于 1,3-偶极环加成反应的成熟方案。通过电泳研究与分子对接相结合，确定了化合物的嵌入性质，同时评估了它们对五种癌细胞系的抗肿瘤活性。所得化合物对银离子也具有良好的亲和力；异恶唑啉环上的 2-羟苄基取代基确保了良好的亲和力和选择性。
