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Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy.

ABSTRACT: 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 IC₅₀ = 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 H₂O₂ decomposition to generate toxic ˙OH which induces apoptosis through CDK-2 inactivation.

SUBMITTER: Cheng Q

PROVIDER: S-EPMC9036967 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy.

Cheng Qianya Q Zhou Tong T Xia Qing Q Lu Xiulian X Xu Heng H Hu Ming M Jing Su S

RSC advances 20210722 41

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 IC50 = 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 deriv ...[more]

PMID: 35478891

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