Citarella Andrea, Moi Davide, Pinzi Luca, Bonanni Davide, Rastelli Giulio
Department of Life Sciences, University of Modena and Reggio Emilia, Via Campi 103, 41125 Modena, Italy.
ACS Omega. 2021 Aug 20;6(34):21843-21849. doi: 10.1021/acsomega.1c03628. eCollection 2021 Aug 31.
Since the approval of three hydroxamic acid-based HDAC inhibitors as anticancer drugs, such functional groups acquired even more notoriety in synthetic medicinal chemistry. The ability of hydroxamic acids (HAs) to chelate metal ions makes this moiety an attractive metal binding group-in particular, Fe(III) and Zn(II)-so that HA derivatives find wide applications as metalloenzymes inhibitors. In this minireview, we will discuss the most relevant features concerning hydroxamic acid derivatives. In a first instance, the physicochemical characteristics of HAs will be summarized; then, an exhaustive description of the most relevant methods for the introduction of such moiety into organic substrates and an overview of their uses in medicinal chemistry will be presented.
自从三种基于异羟肟酸的组蛋白去乙酰化酶（HDAC）抑制剂获批作为抗癌药物以来，这类官能团在合成药物化学领域声名更甚。异羟肟酸（HAs）螯合金属离子的能力使该部分成为有吸引力的金属结合基团，尤其是铁（III）和锌（II），因此HA衍生物作为金属酶抑制剂有广泛应用。在本综述中，我们将讨论异羟肟酸衍生物的最相关特征。首先，将总结HAs的物理化学特性；然后，将详尽描述将此类部分引入有机底物的最相关方法，并概述它们在药物化学中的用途。
