Biological activity of dihydropyrimidinone (DHPM) derivatives: A systematic review

被引：176

作者：

Santana Matos, Larizza Hellen ^{[1
]}

Masson, Flavia Teixeira ^{[1
]}

Simeoni, Luiz Alberto ^{[1
]}

Homem-de-Mello, Mauricio ^{[1
]}

机构：

[1] Univ Brasilia, Hlth Sci Sch, Dept Pharmaceut Sci, Brasilia, DF, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 143卷

关键词：

Dihydropyrimidinones; Monastrol; Toxicity; Cytotoxicity; Biological activity; Systematic review; CALCIUM-CHANNEL BLOCKERS; MICROWAVE-ASSISTED SYNTHESIS; MITOTIC KINESIN EG5; ANHYDRASE INHIBITORY PROPERTIES; MONASTROL-DERIVED COMPOUND; BIPOLAR SPINDLE FORMATION; SMALL-MOLECULE INHIBITOR; SOLVENT-FREE SYNTHESIS; IN-VITRO ANTICANCER; ONE-POT SYNTHESIS;

D O I：

10.1016/j.ejmech.2017.10.073

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2017 Elsevier Masson SAS. All rights reserved.

引用

页码：1779 / 1789

页数：11

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