Molecular Modeling Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.
Molecular Modeling Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.
Eur J Med Chem. 2014 Sep 12;84:206-39. doi: 10.1016/j.ejmech.2014.07.013. Epub 2014 Jul 5.
Flavones have antioxidant, anti-proliferative, anti-tumor, anti-microbial, estrogenic, acetyl cholinesterase, anti-inflammatory activities and are also used in cancer, cardiovascular disease, neurodegenerative disorders, etc. Also, flavonoids are found to have an effect on several mammalian enzymes like protein kinases that regulate multiple cell signaling pathways and alterations in multiple cellular signaling pathways are frequently found in many diseases. Flavones have been an indispensable anchor for the development of new therapeutic agents. The majority of metabolic diseases are speculated to originate from oxidative stress, and it is therefore significant that recent studies have shown the positive effect of flavones on diseases related to oxidative stress. Due to the wide range of biological activities of flavones, their structure-activity relationships have generated interest among medicinal chemists. The outstanding development of flavones derivatives in diverse diseases in very short span of time proves its magnitude for medicinal chemistry research. The present review gives detail about the structural requirement of flavone derivatives for various pharmacological activities. This information may provide an opportunity to scientists of medicinal chemistry discipline to design selective, optimize as well as poly-functional flavone derivatives for the treatment of multi-factorial diseases.
类黄酮具有抗氧化、抗增殖、抗肿瘤、抗菌、雌激素、乙酰胆碱酯酶、抗炎活性，还用于癌症、心血管疾病、神经退行性疾病等。此外，类黄酮被发现对几种哺乳动物酶如蛋白激酶有影响，这些酶调节多种细胞信号通路，而多种细胞信号通路的改变在许多疾病中经常被发现。类黄酮一直是开发新治疗剂不可或缺的基础。大多数代谢疾病被推测源于氧化应激，因此最近的研究表明类黄酮对与氧化应激相关的疾病有积极作用是非常重要的。由于类黄酮具有广泛的生物活性，它们的构效关系引起了药物化学家的兴趣。在很短的时间内，类黄酮衍生物在多种疾病中的出色发展证明了它在药物化学研究中的重要性。本综述详细介绍了类黄酮衍生物对各种药理活性的结构要求。这些信息可能为药物化学领域的科学家提供机会，设计选择性、优化以及多功能类黄酮衍生物，以治疗多因素疾病。
