Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal.
Molecules. 2019 Feb 22;24(4):791. doi: 10.3390/molecules24040791.
Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest in synthetic chiral derivatives of xanthones (CDXs) has been witnessed. The synthetic methodologies can afford structures that otherwise could not be reached within the natural products for biological activity and SAR studies. Another reason that justifies this trend is that both enantiomers can be obtained by using appropriate synthetic pathways, allowing the possibility to perform enantioselectivity studies. In this work, a literature review of synthetic CDXs is presented. The structures, the approaches used for their synthesis and the biological activities are described, emphasizing the enantioselectivity studies.
许多天然存在的黄烷酮都是手性的，具有广泛的生物和药理活性。其中一些已经被深入研究，并通过合成获得。为了获得化合物库用于构效关系（SAR）研究以及提高生物活性，我们以天然原型为灵感，合成了新的具有生物活性的类似物和衍生物。生物活性天然黄烷酮包含了大量结构多样性的化合物，包括各种手性衍生物。因此，最近人们对手性黄烷酮（CDX）的合成衍生物产生了极大的兴趣。合成方法可以提供否则无法从天然产物中获得的结构，用于生物活性和 SAR 研究。另一个证明这一趋势合理的原因是，通过使用适当的合成途径可以获得两种对映异构体，从而有可能进行对映选择性研究。在这项工作中，对合成 CDX 的文献进行了综述。描述了它们的结构、用于合成的方法以及生物活性，强调了对映选择性研究。
