Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions

Yi Dai; Meng Qian; Yan Li

doi:10.3390/molecules28134931

Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions

Molecules. 2023 Jun 22;28(13):4931. doi: 10.3390/molecules28134931.

Authors

Yi Dai^{1

2}, Meng Qian¹, Yan Li¹

Affiliations

¹ College of Pharmaceutical Science, Anhui Xinhua University, Hefei 230088, China.
² Department of Chemistry, University of Science and Technology of China, Hefei 230026, China.

Abstract

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.

Keywords: 7-ethyl-10-hydroxycamptothecin; structural modification; theranostics; tumor targeting.

Publication types

Review

MeSH terms

Antineoplastic Agents, Phytogenic* / pharmacology
Camptothecin
Cell Line, Tumor
Humans
Irinotecan
Neoplasms* / drug therapy
Solubility

Substances

Camptothecin
Irinotecan
Antineoplastic Agents, Phytogenic

Grants and funding

This work was supported by the Natural Science Research Foundation of the Department of Education of Anhui Province (KJ2019A0873), the Scientific Research Team of Anui Xinhua University (No. kytd202211), the Pharmaceutical Institute of Anui Xinhua University (No. yjs202107).