G-quadruplex nucleic acids (G4s) are RNA and DNA secondary structures involved in the regulation of multiple key biological processes. They can be found in telomeres, oncogene promoters, RNAs, but also in viral genomes. Due to their unique structural features, very distinct from the canonical duplexes or single-strands, G4s represent promising pharmacological targets for small molecules, namely G4-ligands. Gold(III) penta-cationic porphyrins, as specific G4 ligands, are able to inhibit HIV-1 infectivity and their antiviral activity correlates with their affinity for G4s. Up to now, one of the best antiviral compounds is meso-5,10,15,20-tetrakis[4-(N-methyl-pyridinium-2-yl)phenyl]porphyrinato gold(III) (1). Starting from this compound, we report a structure/affinity relationship study of gold(III) cationic porphyrins to find out the best porphyrin candidate for functionalization, in order to study the antiviral mechanism of action of these gold(III) porphyrins.

G-四链体核酸 (G4s) 是 RNA 和 DNA 二级结构，参与调节多个关键生物过程。它们可以在端粒、癌基因启动子、RNA 中找到，也可以在病毒基因组中找到。由于其独特的结构特征，与典型的双链体或单链非常不同，G4 代表了小分子（即 G4 配体）的有希望的药理学靶标。Gold(III) 五阳离子卟啉作为特异性 G4 配体，能够抑制 HIV-1 的感染性，其抗病毒活性与其对 G4 的亲和力相关。迄今为止，最好的抗病毒化合物之一是内消旋-5,10,15,20-四[4-( N-甲基-吡啶鎓-2-基)苯基]卟啉金(III)( 1）。从该化合物开始，我们报告了金（III）阳离子卟啉的结构/亲和关系研究，以找出最佳的卟啉候选物进行功能化，以研究这些金（III）卟啉的抗病毒作用机制。