169751-73-9Relevant articles and documents
Gene coding compound library starting head fragment compound and application thereof in gene coding compound library synthesis
-
Paragraph 0059-0061, (2021/11/14)
The invention provides a gene coding compound library starting head fragment compound and application thereof in synthesis of a gene coding compound library, and has good universality. The method is mild in condition, convenient to operate and high in yie
Discovery and biological evaluation of proteolysis targeting chimeras (PROTACs) as an EGFR degraders based on osimertinib and lenalidomide
He, Kailun,Wang, Wenbing,Wang, Xiaoju,Zhang, Xingxian,Zhang, Zhuo,Zheng, Xiaoliang
, (2020/04/21)
Epidermal growth factor receptor (EGFR) is one of the important and valuable drug targets. Overexpression of EGFR is associated with the development of many types of cancer. In this study, three PROTACs small molecules (16a–16c) were designed, synthesized and evaluated for their cytotoxicity against the growth in different NSCLC cell line and the degradation effect. The bioassay results indicated that 16c has a good inhibition in PC9 cells and H1975 cells, and the corresponding IC50 value was 0.413 μM and 0.657 μM, respectively. Western blotting results demonstrated that compound 16c could serve as an effective EGFRdel19-targeting degrader in PC9 cells.
Lenalidomide-based small-molecular compound targeting to EGFR protein degradation, and preparation and application thereof
-
Paragraph 0050; 0061; 0068; 0069; 0070, (2020/09/09)
The invention relates to a lenalidomide-based small-molecular compound targeting to EGFR protein degradation, and preparation and application thereof, and provides a compound targeting to ubiquitination induced EGFR protein degradation and shown as a form
AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF
-
Paragraph 0369-0371; 0414-0416, (2020/01/31)
The present invention aims to provide a compound that: has an excellent cytotoxic action on cancer cells, excellent induction of BET protein degradation in cancer cells, and an excellent binding-inhibiting action on BET protein and acetylated histone; and is effective as an anti-cancer agent, a BET protein degradation-inducing agent, or a BET protein inhibiting agent. A compound indicated in general formula (I) or a pharmacologically acceptable salt thereof. {In the formula, each symbol is as outlined in the Description.}
Atorvastatin Derived HMG-CoA Reductase Degradation Inducing Compound
-
Paragraph 0509-0512, (2020/12/01)
The present invention relates to a HMG-CoA reductase degradation-inducing compound and, more specifically, to a bifunctional compound in which atorvastatin and E3 ubiquitin ligase binding moiety are chemically linked as HMG-CoA reductase binding moiety, to a production method thereof, to a HMG-CoA reductase degradation method using the same, and to a pharmaceutical composition for preventing or treating HMG-CoA reductase-related diseases, comprising the same.
Compound for targeted ubiquitin degradation of EGFR protein as well as pharmaceutical composition and application thereof
-
Paragraph 0043; 0061-0062, (2019/07/04)
The invention discloses a compound for targeted ubiquitin degradation of EGFR protein or a pharmaceutically acceptable salt thereof, and also discloses a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof and
Identification and Characterization of von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Crew, Andrew P.,Raina, Kanak,Dong, Hanqing,Qian, Yimin,Wang, Jing,Vigil, Dominico,Serebrenik, Yevgeniy V.,Hamman, Brian D.,Morgan, Alicia,Ferraro, Caterina,Siu, Kam,Neklesa, Taavi K.,Winkler, James D.,Coleman, Kevin G.,Crews, Craig M.
, p. 583 - 598 (2018/02/07)
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young, the potential for this modality to become a differentiated and therapeutic reality is strong, such that both academic and pharmaceutical institutions are now entering this interesting area of research. In this article, we describe a broadly applicable process for identifying degrader hits based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) and have generalized the key structural elements associated with degradation activities. Compound 3i is a potent hit (TBK1 DC50 = 12 nM, Dmax = 96%) with excellent selectivity against a related kinase IKK?, which was further used as a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells.
COMPOUNDS FOR THE MODULATION OF RIP2 KINASE ACTIVITY
-
, (2017/04/11)
The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
Antithrombotic compound
-
, (2008/06/13)
The present invention relates compounds of the formula Aoligosaccharide-spacer-GpIIb/IIIa antagonist wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensa
Synthese von massgeschneiderten Glycokonjugaten, die AT-III-vermittelt die Blutgerinnungsfaktoren Xa und Thrombin inhibieren
Westerduin, Pieter,Basten, Jan E. M.,Broekhoven, Marc A.,Kimpe, Vera de,Kuijpers, Will H. A.,Boeckel, Constant A. A.
, p. 339 - 342 (2007/10/03)
Keywords: Antithrombotica; Enzyminhibitoren; Heparin
