70938-59-9Relevant articles and documents
Discovery of 4′-O-methylscutellarein as a potent SARS-CoV-2 main protease inhibitor
Li, Maotian,Li, Yingxia,Wang, Yujie,Wu, Qianqian,Xiao, Yibei,Yan, Shiqiang
, p. 76 - 82 (2022/03/23)
The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has resulted in millions of deaths and seriously threatened public health and safety. Despite COVID-19 vaccines being readily popularized worldwide, targeted therapeutic agents for the treatment of this disease remain very limited. Here, we studied the inhibitory activity of the scutellarein and its methylated derivatives against SARS-CoV-2 main protease (Mpro) by the fluorescence resonance energy transfer (FRET) assay. Among all the methylated derivatives we studied, 4′-O-methylscutellarein exhibited the most promising enzyme inhibitory activity in vitro, with the half-maximal inhibitory concentration value (IC50) of 0.40 ± 0.03 μM. Additionally, the mechanism of action of the hits was further characterized through enzyme kinetic studies and molecular docking. Overall, our results implied that 4′-O-methylscutellarein could be a primary lead compound with clinical potential for the development of inhibitors against the SARS-CoV-2 Mpro.
Scutellarin amide derivative, and preparation method and application thereof
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Paragraph 0018; 0029-0031; 0032-0034, (2020/09/16)
The invention discloses a scutellarin amide derivative, and a preparation method and application thereof, and belongs to the field of natural medicines and medicinal chemistry. The scutellarin derivative and the pharmaceutically acceptable salt thereof have structures shown as the following general formula I. The scutellarin derivative is prepared by amidation at a carbohydrate carboxyl site and is applied to preparation of anti-tumor drugs. Good anti-tumor cell proliferation effects are achieved.
Furazan type NO (nitric oxide) donor scutellarin derivative with anti-tumor activity and preparation method and application thereof
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Paragraph 0024; 0025; 0026; 0027, (2017/08/31)
The invention relates to the field of natural medicines and medicine chemistry, in particular to a furazan type NO (nitric oxide) donor scutellarin derivative with anti-tumor activity and a pharmaceutically acceptable salt thereof, and in particular to a furazan type NO donor-substituted scutellarin derivative with a piperazine ringfatty chain link arm on saccharide carboxyl sites and a preparation method and application thereof in preparing anti-tumor medicines. The structures of the furazan type NO donor scutellarin derivative with anti-tumor activity and the pharmaceutically acceptable salt thereof are shown in the formula I, wherein R and n R1 are described in the right claim and instructiondescription. The formula I is shown in the descriptionattached figure.