Jiang Xueyang, Li Siyi, Wang Ning, Li Jiaming
Department of Medicinal Chemistry, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China.
Department of Medicinal Chemistry, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China; Anhui Province Key Laboratory of Research & Development of Chinese Medicine, Hefei, China; Institute for Pharmacodynamics and Safety Evaluation of Chinese Medicine, Anhui Academy of Traditional Chinese Medicine, Hefei 230012 China.
Bioorg Med Chem. 2025 Apr 15;121:118110. doi: 10.1016/j.bmc.2025.118110. Epub 2025 Feb 11.
Ligustrazine has gained significant attention for its unique structural role in natural medicinal chemistry and its potential in drug discovery and development. The ligustrazine structure has been recognized as a clinical drug for treating cardiovascular and cerebrovascular diseases, especially in the design of neuroprotective agents. Recently, ligustrazine-based anti-tumor agents have also been reported. This knowledge can undoubtedly be applied to design multi-target-directed ligands, a highly relevant strategy for the complex pathological conditions of multifactorial diseases. In this review, we first discuss the biological properties and clinical applications of ligustrazine, then focus on the rational design of ligustrazine-based multifunctional ligands.
川芎嗪因其在天然药物化学中的独特结构作用以及在药物发现与开发中的潜力而备受关注。川芎嗪结构已被公认为是一种治疗心脑血管疾病的临床药物,尤其是在神经保护剂的设计方面。最近,基于川芎嗪的抗肿瘤药物也有报道。这些知识无疑可应用于设计多靶点导向配体,这是针对多因素疾病复杂病理状况的一种高度相关策略。在本综述中,我们首先讨论川芎嗪的生物学特性和临床应用,然后重点关注基于川芎嗪的多功能配体的合理设计。