Matos Larizza Hellen Santana, Masson Flávia Teixeira, Simeoni Luiz Alberto, Homem-de-Mello Mauricio
Department of Pharmaceutical Sciences, Health Sciences School, University of Brasilia, Brazil.
Department of Pharmaceutical Sciences, Health Sciences School, University of Brasilia, Brazil.
Eur J Med Chem. 2018 Jan 1;143:1779-1789. doi: 10.1016/j.ejmech.2017.10.073. Epub 2017 Oct 31.
Dihydropyrimidinones are heterocycles with a pyrimidine moiety in the ring nucleus, which, in recent decades, have aroused interest in medicinal chemistry due to alleged versatile biological activity. In this systematic review, we describe the currently published activities of dihydropyrimidinone derivatives. Between 1990 and December 31st, 2016, 115 articles outlined biological activities or toxicity of DHPM derivatives, 12 of those involved in vivo experiments. The main activities associated with this class of compounds are antitumoral (43 articles), anti-inflammatory (12 articles), antibacterial (20 articles) and calcium channel antagonism/inhibition (14 articles). Antitumoral activity is the main biological property evaluated, since the main representative compound of this class (monastrol) is a known Eg5 kinesin inhibitor. This review depicts a variety of other pharmacological activities associated with DHPM derivatives, but the main findings are essentially in vitro characteristics of the substances. This review presents the current state of the art of DHPM biological activities and demonstrates that there is still a need for further in vivo studies to better delineate the pharmacological potential of this class of substances.
二氢嘧啶酮是一类在环核中含有嘧啶部分的杂环化合物，近几十年来，因其据称具有多种生物活性而引起了药物化学领域的关注。在本系统综述中，我们描述了目前已发表的二氢嘧啶酮衍生物的活性。在1990年至2016年12月31日期间，有115篇文章概述了二氢嘧啶酮衍生物的生物活性或毒性，其中12篇涉及体内实验。与这类化合物相关的主要活性包括抗肿瘤（43篇文章）、抗炎（12篇文章）、抗菌（20篇文章）以及钙通道拮抗/抑制（14篇文章）。抗肿瘤活性是评估的主要生物学特性，因为这类化合物的主要代表性化合物（monastrol）是一种已知的驱动蛋白Eg5抑制剂。本综述描述了与二氢嘧啶酮衍生物相关的多种其他药理活性，但主要发现基本上是这些物质的体外特性。本综述展示了二氢嘧啶酮生物活性的当前研究现状，并表明仍需要进一步的体内研究，以更好地描绘这类物质的药理潜力。
