College of Pharmaceutical Science, Anhui Xinhua University, Hefei 230088, China.
Department of Chemistry, University of Science and Technology of China, Hefei 230026, China.
Molecules. 2023 Jun 22;28(13):4931. doi: 10.3390/molecules28134931.
As a camptothecin derivative, 7-ethyl-10-hydroxycamptothecin (SN38) combats cancer by inhibiting topoisomerase I. SN38 is one of the most active compounds among camptothecin derivatives. In addition, SN38 is also a theranostic reagent due to its intrinsic fluorescence. However, the poor water solubility, high systemic toxicity and limited action against drug resistance and metastasis of tumor cells of SN38 indicates that there is great space for the structural modification of SN38. From the perspective of chemical modification, this paper summarizes the progress of SN38 in improving solubility, increasing activity, reducing toxicity and possessing multifunction and analyzes the strategies of structure modification to provide a reference for drug development based on SN38.
作为喜树碱的衍生物，7-乙基-10-羟基喜树碱（SN38）通过抑制拓扑异构酶 I 来对抗癌症。SN38 是喜树碱衍生物中最具活性的化合物之一。此外，由于其固有荧光，SN38 也是一种治疗诊断试剂。然而，SN38 的水溶性差、全身毒性高以及对肿瘤细胞耐药性和转移的作用有限表明，SN38 的结构修饰仍有很大的空间。从化学修饰的角度来看，本文综述了提高 SN38 溶解度、增加活性、降低毒性和具有多功能性的研究进展，并分析了结构修饰的策略，为基于 SN38 的药物开发提供参考。
