Georgiou Eleftheria A, Paraskevas Konstantinos, Koutra Christina, Persoons Leentje, Schols Dominique, De Jonghe Steven, Kostakis Ioannis K
Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece.
Department of Pharmacy, Division of Pharmacognosy and Natural Products Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece.
Molecules. 2024 Nov 25;29(23):5549. doi: 10.3390/molecules29235549.
Thirteen new 4,7-disubstituted pyrimido[4,5-]pyrimidines were synthesized via a straightforward methodology starting from thiourea. The anti-proliferative activity of these compounds was evaluated across a diverse panel of eight cancer cell lines, with derivatives and showing efficacy against several hematological cancer types. Furthermore, all compounds were assessed for their antiviral potency against a panel of viruses. Compounds featuring a cyclopropylamino group and an aminoindane moiety exhibited remarkable efficacy against human coronavirus 229E (HCoV-229E). These findings highlight the pyrimidino[4,5-]pyrimidine scaffold as an interesting framework for the design of novel antiviral agents against HCoVs, with compounds , , and emerging as strong candidates for further investigation.
通过一种从硫脲出发的直接方法合成了13种新的4,7-二取代嘧啶并[4,5 -]嘧啶。在一组多样的8种癌细胞系中评估了这些化合物的抗增殖活性，衍生物 和 对几种血液系统癌症类型显示出疗效。此外，还评估了所有化合物对一组病毒的抗病毒效力。具有环丙基氨基和氨基茚部分的化合物对人冠状病毒229E（HCoV - 229E）表现出显著疗效。这些发现突出了嘧啶并[4,5 -]嘧啶骨架作为设计针对HCoV的新型抗病毒药物的一个有趣框架，化合物 、 和 成为进一步研究的有力候选物。
