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Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions
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 solubi...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10343627/ https://www.ncbi.nlm.nih.gov/pubmed/37446591 http://dx.doi.org/10.3390/molecules28134931 |
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author | Dai, Yi Qian, Meng Li, Yan |
author_facet | Dai, Yi Qian, Meng Li, Yan |
author_sort | Dai, Yi |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-10343627 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-103436272023-07-14 Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions Dai, Yi Qian, Meng Li, Yan Molecules Review 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. MDPI 2023-06-22 /pmc/articles/PMC10343627/ /pubmed/37446591 http://dx.doi.org/10.3390/molecules28134931 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Dai, Yi Qian, Meng Li, Yan Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions |
title | Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions |
title_full | Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions |
title_fullStr | Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions |
title_full_unstemmed | Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions |
title_short | Structural Modification Endows Small-Molecular SN38 Derivatives with Multifaceted Functions |
title_sort | structural modification endows small-molecular sn38 derivatives with multifaceted functions |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10343627/ https://www.ncbi.nlm.nih.gov/pubmed/37446591 http://dx.doi.org/10.3390/molecules28134931 |
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