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 NO-donating scutellarin derivative with anti-tumor activity, and preparation method and application thereof
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Paragraph 0023; 0024; 0025; 0026; 0027; 0028, (2017/07/19)
The invention relates to the field of natural medicine and medicinal chemistry, in particular to a furazan NO-donating scutellarin derivative with anti-tumor activity, and a pharmaceutically acceptable salt thereof. The invention specifically relates to the furazan NO-donating substituted scutellarin derivatives with an aliphatic chain connecting arm on uronic acid base loci, and application for preparing anti-tumor drugs. The structures of the furazan NO-donating scutellarin derivative and the pharmaceutically acceptable salt thereof are shown in the following general formula I, wherein R and R1 are disclosed in claims and specifications. The formula is shown in the specification.