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Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy
In the current study, six ferrocenylseleno-dopamine derivatives with different structural parameters were designed. Among these derivatives, F4b, containing two ferrocene units and a tertiary amine, showed in vitro anticancer activity with IC(50) = 2.4 ± 0.4 μM for MGC-803 cells, and its in vivo stu...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9036967/ https://www.ncbi.nlm.nih.gov/pubmed/35478891 http://dx.doi.org/10.1039/d1ra03537a |
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author | Cheng, Qianya Zhou, Tong Xia, Qing Lu, Xiulian Xu, Heng Hu, Ming Jing, Su |
author_facet | Cheng, Qianya Zhou, Tong Xia, Qing Lu, Xiulian Xu, Heng Hu, Ming Jing, Su |
author_sort | Cheng, Qianya |
collection | PubMed |
description | In the current study, six ferrocenylseleno-dopamine derivatives with different structural parameters were designed. Among these derivatives, F4b, containing two ferrocene units and a tertiary amine, showed in vitro anticancer activity with IC(50) = 2.4 ± 0.4 μM for MGC-803 cells, and its in vivo studies suggested effective antitumor activity in mice bearing an MGC-803 tumor xenograft. Mechanistic study revealed that the cytotoxicity of these ferrocenylseleno-dopamine derivatives is mainly related to the Fenton-like reaction under physiological conditions, and the tertiary amine in F4b can facilitate the H(2)O(2) decomposition to generate toxic ˙OH which induces apoptosis through CDK-2 inactivation. |
format | Online Article Text |
id | pubmed-9036967 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-90369672022-04-26 Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy Cheng, Qianya Zhou, Tong Xia, Qing Lu, Xiulian Xu, Heng Hu, Ming Jing, Su RSC Adv Chemistry In the current study, six ferrocenylseleno-dopamine derivatives with different structural parameters were designed. Among these derivatives, F4b, containing two ferrocene units and a tertiary amine, showed in vitro anticancer activity with IC(50) = 2.4 ± 0.4 μM for MGC-803 cells, and its in vivo studies suggested effective antitumor activity in mice bearing an MGC-803 tumor xenograft. Mechanistic study revealed that the cytotoxicity of these ferrocenylseleno-dopamine derivatives is mainly related to the Fenton-like reaction under physiological conditions, and the tertiary amine in F4b can facilitate the H(2)O(2) decomposition to generate toxic ˙OH which induces apoptosis through CDK-2 inactivation. The Royal Society of Chemistry 2021-07-22 /pmc/articles/PMC9036967/ /pubmed/35478891 http://dx.doi.org/10.1039/d1ra03537a Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
spellingShingle | Chemistry Cheng, Qianya Zhou, Tong Xia, Qing Lu, Xiulian Xu, Heng Hu, Ming Jing, Su Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy |
title | Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy |
title_full | Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy |
title_fullStr | Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy |
title_full_unstemmed | Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy |
title_short | Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy |
title_sort | design of ferrocenylseleno-dopamine derivatives to optimize the fenton-like reaction efficiency and antitumor efficacy |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9036967/ https://www.ncbi.nlm.nih.gov/pubmed/35478891 http://dx.doi.org/10.1039/d1ra03537a |
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