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.

二氢嘧啶酮是在环核中具有嘧啶部分的杂环，由于据称具有多种生物活性，近几十年来引起了人们对药物化学的兴趣。在此系统的审查中，我们描述了二氢嘧啶酮衍生物的当前公开的活动。在1990年至2016年12月31日期间，共有115篇文章概述了DHPM衍生物的生物学活性或毒性，其中12篇涉及体内实验。与这类化合物相关的主要活性是抗肿瘤（43篇文章），抗炎（12篇文章），抗菌（20篇文章）和钙通道拮抗/抑制（14篇文章）。抗肿瘤活性是评估的主要生物学特性，因为此类的主要代表化合物（monastrol）是已知的Eg5驱动蛋白抑制剂。这篇综述描述了与DHPM衍生物有关的多种其他药理活性，但主要发现实质上是该物质的体外特性。这项审查介绍了DHPM生物活性的最新技术水平，并表明仍然需要进一步的体内 更好地描述此类药物的药理潜力的研究。