Shaanxi University of Chinese Medicine, Xianyang, Shaanxi Province, 712046, PR China.
Shaanxi University of Chinese Medicine, Xianyang, Shaanxi Province, 712046, PR China.
Eur J Med Chem. 2022 Dec 5;243:114733. doi: 10.1016/j.ejmech.2022.114733. Epub 2022 Sep 3.
Baicalein (5,6,7-trihydroxyflavone) and wogonin (5,7-dihydroxy-8-methoxyflavone), as typical flavonoids isolated from Scutellaria baicalensis, are well important precursors in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have synthesized baicalein and wogonin derivatives with multiple medicinal properties including antitumor, central nervous system (CNS), anti-inflammatory, antiviral, antimicrobial and hypoglycemic activities. Simultaneously, SAR (Structure-Activity Relationship) analysis has been gradually possessed, along with a great deal of derivatives have been derived for potential targets. In this article, we comprehensively summarize the biological activities and SAR for baicalein and wogonin derivatives, along with the featuring bioactive molecules reported in patents, wishing to provide an overall retrospect and prospect on baicalein and wogonin analogues.
黄芩素（5,6,7-三羟基黄酮）和汉黄芩素（5,7-二羟基-8-甲氧基黄酮），作为从黄芩中分离得到的典型黄酮类化合物，是药物发现中非常重要的前体物质，在药理学实践中产生了多种治疗相关的应用。药物化学领域的研究已经合成了具有多种药理活性的黄芩素和汉黄芩素衍生物，包括抗肿瘤、中枢神经系统（CNS）、抗炎、抗病毒、抗菌和降血糖活性。同时，SAR（构效关系）分析逐渐得到了发展，大量的衍生物被开发出来用于潜在的靶点。在本文中，我们全面总结了黄芩素和汉黄芩素衍生物的生物活性和 SAR，以及专利中报道的具有特色的生物活性分子，希望对黄芩素和汉黄芩素类似物进行全面的回顾和展望。
