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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...

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Autores principales: Cheng, Qianya, Zhou, Tong, Xia, Qing, Lu, Xiulian, Xu, Heng, Hu, Ming, Jing, Su
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
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.
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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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