Nath Rajarshi, Manna Swarup, Panda Shambo, Maity Arindam, Bandyopadhyay Krishnalekha, Das Arijit, Khan Shah Alam, Debnath Biplab, Akhtar Md Jawaid
Department of Pharmacy, Bharat Technology, Howrah, West Bengal, Uluberia, 711316, India.
Department of Pharmaceutical Technology, JIS University, Agarpara Campus, Nilgunj Road, Kolkata-109, Agarpara, KOL-81, India.
Chem Biodivers. 2025 Mar;22(3):e202401899. doi: 10.1002/cbdv.202401899. Epub 2024 Nov 14.
The toxicity associated with synthetic drugs used for treating various diseases is common. This led to a growing interest in searching and incorporating natural functional core structures such as flavonoid and their derivatives via chemical modifications to overcome the toxicity problems and enhance their biological spectrum. Natural core structures such as flavonoids are accepted due to their safety to the environment and owing to their varieties of biological activities such as anti-Alzheimer, antimicrobial, anticancer, anti-inflammatory, antidiabetics, and antiviral properties. Based on their chemical structure, flavonoids are classified into various classes such as flavone, flavanol, flavanone, isoflavone, and Anthocyanin, etc. The present review focuses on the potential role of the flavonoid ring-containing derivatives, highlighting their ability to prevent and treat non-communicable diseases such as diabetes, Alzheimer's, and cancer. The pharmacological activities of the flavonoid's derivatives are mainly attributed to their antioxidant effects against free radicals, and reactive oxygen species as well as their ability to act as enzymes inhibitors. The review covers the synthetic strategies of flavonoid derivatives, structure activity relationship (SAR), and in silico studies to improve the efficacy of these compounds. The SAR, molecular docking analysis will enable medicinal chemists to search further, develop potent and newer therapeutic agents.
用于治疗各种疾病的合成药物所具有的毒性很常见。这使得人们越来越有兴趣通过化学修饰来寻找并纳入天然功能核心结构，如黄酮类及其衍生物，以克服毒性问题并扩大其生物活性谱。诸如黄酮类等天然核心结构因其对环境的安全性以及其多种生物活性，如抗阿尔茨海默病、抗菌、抗癌、抗炎、抗糖尿病和抗病毒特性而被认可。基于其化学结构，黄酮类被分为不同类别，如黄酮、黄烷醇、黄烷酮、异黄酮和花青素等。本综述重点关注含黄酮环衍生物的潜在作用，突出其预防和治疗糖尿病、阿尔茨海默病和癌症等非传染性疾病的能力。黄酮类衍生物的药理活性主要归因于其对自由基和活性氧的抗氧化作用以及作为酶抑制剂的能力。该综述涵盖了黄酮类衍生物的合成策略、构效关系（SAR）以及计算机模拟研究，以提高这些化合物的疗效。构效关系、分子对接分析将使药物化学家能够进一步探索，开发出强效且更新的治疗药物。
