Lu Yuzhi, Li Jun, Dong Chun-E, Huang Jian, Zhou Hai-Bing, Wang Wei
Hubei Province Engineering & Technology Research Center for Fluorinated Pharmaceuticals, Key Laboratory of Combinatorial Biosynthesis & Drug Discovery, Ministry of Education, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China.
College of Life Sciences, Wuhan University, Wuhan 430072, China.
Future Med Chem. 2017 Jul;9(11):1243-1275. doi: 10.4155/fmc-2017-0046. Epub 2017 Jul 19.
Gossypol as a natural occurring polyphenol has been studied in a wide range of therapeutic contexts for a long time. The chemical modifications on gossypol were limited due to the unique chemical properties of polyphenols. The design and synthesis of gossypol derivatives and the exploration of their biological activities are the interest of the synthetic chemists, medicinal chemists and pharmacologists. Thus, the progress of diverse gossypol derivatives and analogs' synthesis, biological activities, mechanism elucidation and drug discovery based on gossypol scaffold is summarized.
棉酚作为一种天然存在的多酚,长期以来一直在广泛的治疗背景下进行研究。由于多酚独特的化学性质,对棉酚的化学修饰受到限制。棉酚衍生物的设计与合成及其生物活性的探索是合成化学家、药物化学家和药理学家感兴趣的领域。因此,本文综述了基于棉酚骨架的各种棉酚衍生物和类似物的合成、生物活性、作用机制阐明及药物发现方面的进展。