Design of ferrocenylseleno-dopamine derivatives to optimize the Fenton-like reaction efficiency and antitumor efficacy. Issue 41 (22nd July 2021)

• Record Type: Journal Article
• Authors: Cheng, Qianya; Zhou, Tong; Xia, Qing; Lu, Xiulian; Xu, Heng; Hu, Ming; Jing, Su
• Is Part Of: RSC advances. Volume 11:Issue 41(2021)
• Page Start: 25477
• Page End: 25483
• Publication Date: 2021-07-22
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d1ra03537a
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : The tertiary amine in F4b facilitates the Fenton-like reaction to generate toxic ˙OH which induces apoptosis through CDK-2 inactivation. 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 H2 O2 decomposition to generate toxic ˙OH which induces apoptosis through CDK-2 inactivation.