204847-08-5Relevant articles and documents
2-furanyl-quinoline-4-formamide compound and application thereof
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Paragraph 0018-0020, (2021/02/06)
The invention discloses a 2-furanyl-quinoline-4-formamide compound and application thereof, and the structural formula of the 2-furanyl-quinoline-4-formamide compound is shown as a formula (4) in thespecification, wherein R1 is selected from H, halogen or
Quinoline-4-carboxamide skeleton derivative and application thereof
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Paragraph 0048-0051; 0072-0075, (2021/06/09)
The invention discloses a quinoline-4-formamide skeleton derivative and application thereof, belonging to the field of chemical medicines. The invention provides a compound as shown in a formula I or pharmaceutically acceptable salt thereof. The invention
Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity
Chen, Xiuli,Sun, Weining,Huang, Shenzhen,Zhang, Hailin,Lin, Guifeng,Li, Hui,Qiao, Jingxin,Li, Linli,Yang, Shengyong
, p. 10474 - 10495 (2020/11/02)
SIRT6 activation is thought to be a promising target for the treatment of many diseases, particularly cancer. Herein, we report the discovery of a series of new small-molecule SIRT6 activators. Structure-activity relationship analyses led to the identific
SMALL MOLECULE INHIBITORS OF APOBEC3G AND APOBEC3B
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Page/Page column 38, (2015/07/23)
The present invention is directed to compositions and methods for inhibition of APOBEC-related DNA cytosine deaminase enzymes, and to methods of using the compounds for treatment of a disease in a patient, such as an infectious disease or a cancer. The in
Oxidative Reactivities of 2-Furylquinolines: Ubiquitous Scaffolds in Common High-Throughput Screening Libraries
Olson, Margaret E.,Abate-Pella, Daniel,Perkins, Angela L.,Li, Ming,Carpenter, Michael A.,Rathore, Anurag,Harris, Reuben S.,Harki, Daniel A.
, p. 7419 - 7430 (2015/10/05)
High-throughput screening (HTS) was employed to discover APOBEC3G inhibitors, and multiple 2-furylquinolines (e.g., 1) were found. Dose-response assays with 1 from the HTS sample, as well as commercial material, yielded similar confirmatory results. Interestingly, freshly synthesized and DMSO-solubilized 1 was inactive. Repeated screening of the DMSO aliquot of synthesized 1 revealed increasing APOBEC3G inhibitory activity with age, suggesting that 1 decomposes into an active inhibitor. Laboratory aging of 1 followed by analysis revealed that 1 undergoes oxidative decomposition in air, resulting from a [4 + 2] cycloaddition between the furan of 1 and 1O2. The resulting endoperoxide then undergoes additional transformations, highlighted by Baeyer-Villager rearrangements, to deliver lactam, carboxylic acid, and aldehyde products. The endoperoxide also undergoes hydrolytic opening followed by further transformations to a bis-enone. Eight structurally related analogues from HTS libraries were similarly reactive. This study constitutes a cautionary tale to validate 2-furylquinolines for structure and stability prior to chemical optimization campaigns.
CYTOSINE DEAMINASE MODULATORS FOR ENHANCEMENT OF DNA TRANSFECTION
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Page/Page column 67, (2013/06/05)
Compounds and methods are provided for enhancing or boosting the transfection rate or efficiency of mammalian cells by foreign DNA, such as bacterial plasmid DNA. Compounds, including natural products and inventive synthetic compounds can increase the effectiveness of uptake and incorporation of foreign DNA by mammalian cells, such as human cells, by suppression of DNA cytosine deamination, which is believed to be a mechanism by which these cells eliminate foreign DNA. Inhibition of the cytosine deaminase enzymes by compounds as described herein serves to provide more effective transfection of eukaryotic cells by plasmids including engineered gene sequences. Transfection can be used to study cellular processes, or to cure genetic diseases in human patients. The inventive materials and methods increase the efficiency and effectiveness of such transfection techniques.