Teaching and Research Office of Analytical Chemistry, School of Pharmaceutical Sciences, Guizhou University of Traditional Chinese Medicine, Guizhou, China.
Arch Pharm (Weinheim). 2020 Mar;353(3):e1900299. doi: 10.1002/ardp.201900299. Epub 2020 Jan 27.
Dimerization is a promising strategy to develop novel drug candidates that could extend the biological spectrum, enhance the activity, overcome drug resistance, as well as improve pharmacological, pharmacokinetic, and physicochemical profiles. Isatin dimers possess a broad spectrum of biological properties and the isatin dimer indirubin has already been used in the clinic, revealing the potential of isatin dimers as putative drugs. This review covers the recent advances of isatin dimers as pharmacologically significant scaffolds and the structure-activity relationship to set up the direction for the design and development of isatin dimers with higher efficiency and lower toxicity.
二聚化是一种有前途的策略，可以开发新的药物候选物，这些候选物可以扩展生物谱、增强活性、克服耐药性，并改善药理学、药代动力学和物理化学特性。色胺二聚体具有广泛的生物特性，色胺二聚体靛玉红已在临床上使用，显示出色胺二聚体作为潜在药物的潜力。本文综述了色胺二聚体作为具有药理意义的支架的最新进展，以及构效关系，为设计和开发具有更高效率和更低毒性的色胺二聚体指明了方向。
