LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
CICECO-Aveiro Institute of Materials, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
Molecules. 2020 Mar 17;25(6):1364. doi: 10.3390/molecules25061364.
The present review presents an overview of antitumor pyrazoles of natural or bioinspired origins. Pyrazole compounds are relatively rare in nature, the first ones having been reported in 1966 and being essentially used as somniferous drugs. Cytotoxic pyrazoles of natural sources were first isolated in 1969, and a few others have been reported since then, most of them in the last decade. This paper presents a perspective on the current knowledge on antitumor natural pyrazoles, organized into two sections. The first focuses on the three known families of cytotoxic pyrazoles that were directly isolated from plants, for which the knowledge of the medicinal properties is in its infancy. The second section describes pyrazole derivatives of natural products, discussing their structure-activity relationships.
本综述概述了天然或生物灵感来源的抗肿瘤吡唑类化合物。吡唑类化合物在自然界中相对较少,最早的吡唑类化合物于 1966 年被报道,主要用作催眠药物。天然来源的细胞毒性吡唑类化合物于 1969 年首次被分离出来,此后又有一些被报道,其中大部分是在过去十年中。本文综述了抗肿瘤天然吡唑类化合物的最新研究进展,分为两部分。第一部分重点介绍了从植物中直接分离出来的三种已知的细胞毒性吡唑类化合物家族,对这些化合物的药用特性的了解还处于起步阶段。第二部分描述了天然产物的吡唑衍生物,讨论了它们的结构-活性关系。