An efficient and convenient microwave-assisted chemical synthesis of (thio)xanthones with additional in vitro and in silico characterization
作者:Donatella Verbanac、Subhash C. Jain、Nidhi Jain、Mahesh Chand、Hana Čipčić Paljetak、Mario Matijašić、Mihaela Perić、Višnja Stepanić、Luciano Saso
DOI:10.1016/j.bmc.2012.03.074
日期:2012.5
chemical scaffold for the synthesis of new drug candidates. One of the main obstacles in utilization of these compounds was related to the difficulties in their chemical synthesis. Most of the known methods require two steps, and are limited to specific reagents not applicable to a large number of starting materials. In this paper a new and improved method for chemical synthesis of xanthones is presented
氧杂蒽酮及其硫代衍生物是一类具有多种药理和生物学活性的多效化合物。尽管这些活动主要是在实验室条件下确定的,但该类本身具有很大的潜力,可以用作有希望的化学支架,用于合成新的候选药物。利用这些化合物的主要障碍之一与它们的化学合成困难有关。大多数已知方法需要两个步骤,并且限于不适用于大量起始材料的特定试剂。本文提出了一种新的和改进的化学合成氧杂蒽酮的方法。通过应用新方法,我们已在较短的反应时间(50 s)和较高的收率(> 80%)。最后,进行了不同细菌种类的初步体外筛选和细胞毒性评估,以及计算机活性评估。获得的结果证实了这类分子的潜在药理学用途。