Yicathins B and C and Analogues: Total Synthesis, Lipophilicity and Biological Activities
作者:Daniela R. P. Loureiro、Álvaro F. Magalhães、José X. Soares、Joana Pinto、Carlos M. G. Azevedo、Sara Vieira、Ana Henriques、Helena Ferreira、Nuno Neves、Hassan Bousbaa、Salette Reis、Carlos M. M. Afonso、Madalena M. M. Pinto
DOI:10.1002/cmdc.201900735
日期:2020.5.6
and exquisite bioactive compounds. Yicathins B and C are two marine-derived xanthones that have shown antibacterial and antifungal activity. Herein, the total synthesis of these yicathins and six novel analogues is reported for the first time. As marine natural products tend to have very lipophilic scaffolds, the lipophilicity of yicathins and their analogues was evaluated in the classical octanol/water
天然产物一直是药物开发中新发现和新发现的重要来源,而海洋环境被认为是新颖而精致的生物活性化合物的重要来源。甲壳素B和C是两种海洋衍生的氧杂蒽酮,具有抗菌和抗真菌活性。在本文中,首次报道了这些叶黄素和六种新的类似物的总合成。由于海洋天然产物倾向于具有非常亲脂的支架,因此在经典的辛醇/水系统和基于仿生模型的系统中评估了腐霉菌素及其类似物的亲脂性。由于黄原核是“特权结构”,因此评估了其他生物学活性,即抗肿瘤和抗炎活性。