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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Detalles Bibliográficos
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:
Chemistry
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
Descripción
Sumario: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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