39753-54-3Relevant academic research and scientific papers
Gold(I)-Mediated Cycloisomerization/Cycloaddition Enables Bioinspired Syntheses of Neonectrolides B-E and Analogues
Purgett, Thomas J.,Dyer, Matthew W.,Bickel, Bryce,McNeely, James,Porco, John A.
, p. 15135 - 15144 (2019)
Development of a synthetic route to the oxaphenalenone (OP) natural products neonectrolides B-E is described. The synthesis relies on gold-catalyzed 6-endo-dig hydroarylation of an unusual enynol substrate as well as a one-pot Rieche formylation/cyclization/deprotection sequence to efficiently construct the tricyclic oxaphenalenone framework in the form of a masked ortho-quinone methide (o-QM). A tandem cycloisomerization/[4 + 2] cycloaddition strategy was employed to quickly construct molecules resembling the neonectrolides. The tricyclic OP natural product SF226 could be converted to corymbiferan lactone E and a related masked o-QM. Our study culminates with the application of the tandem reaction sequence to syntheses of neonectrolides B-E as well as previously unreported exo-diastereomers.
Palladium-Catalyzed 5-exo-dig Cyclization Cascade, Sequential Amination/Etherification for Stereoselective Construction of 3-Methyleneindolinones
Zuo, Youpeng,He, Xinwei,Tang, Qiang,Hu, Wangcheng,Zhou, Tongtong,Hu, Wenbo,Shang, Yongjia
supporting information, p. 2117 - 2123 (2020/12/22)
An cascade intramolecular 5-exo-dig cyclization of N-(2-iodophenyl)propiolamides and sequential amination/etherification (with N-hydroxybenzamides, phenyl hydroxycarbamate) protocol for the synthesis of amino- and phenoxy-substituted 3-methyleneindolinones using unexpensive Pd(PPh3)4 as catalyst has been developed. The protocol enables the assembly of structurally important oxindole cores featuring moderate functional group tolerance (particularly the halo group), affording a broad spectrum of products with diverse substituents in good to excellent yields. (Figure presented.).
INHIBITORS OF CYCLIN-DEPENDENT KINASES
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Paragraph 00282, (2021/02/12)
Provided herein are compounds which are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
INHIBITORS OF CYCLIN-DEPENDENT KINASES
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Paragraph 00605, (2020/01/24)
Provided herein are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Optical isomers of FGFR4 inhibitors, and applications thereof
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Paragraph 0047; 0061-0063, (2020/06/02)
The invention belongs to the field of medical chemistry, relates to optical isomers of a class of FGFR4 inhibitors, and applications thereof, and specifically provides an optical isomer represented bya formula I or a formula II or a hydrate, a solvate, a
Benzimidazole ring-containing propyne amide derivative as well as preparation method and pharmaceutical composition and application thereof
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Paragraph 0138; 0141, (2020/11/13)
The invention relates to a benzimidazole ring-containing propiolamide derivative as shown in the formula I, its medicinal salt and their preparation method, a composition containing one or more of the compounds and an application of the compounds in treating tumor diseases.
PYRROLO-AROMATIC HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
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Paragraph 0127; 0267, (2019/11/11)
The present invention relates to pyrrolo-aromatic heterocyclic compounds, a preparation method therefor and medical use thereof. Particularly, the present invention relates to a compound represented by formula I, a preparation method therefor, a pharmaceu
Thiazole-containing propyne amide derivative as well as preparation method and pharmaceutical composition and application thereof
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Paragraph 0055; 0063; 0064; 0101; 0113; 0114, (2019/10/15)
The invention relates to propynamide derivatives shown in a formula I as well as pharmaceutically acceptable salt and preparation method thereof, a composition containing one or more of the compounds, and an application of the compounds to treatment of tu
Oxazoline-containing propyne amide derivative as well as preparation method and pharmaceutical composition and application thereof
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Paragraph 0063-0064; 0118-0119, (2019/10/15)
The invention relates to propynamide derivatives shown in a formula I as well as pharmaceutically acceptable salt and preparation method thereof, a composition containing one or more of the compounds, and an application of the compounds to treatment of tu
Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors
Rowlands, Rachel A.,Cato, M. Claire,Waldschmidt, Helen V.,Bouley, Renee A.,Chen, Qiuyan,Avramova, Larisa,Larsen, Scott D.,Tesmer, John J. G.,White, Andrew D.
supporting information, p. 1628 - 1634 (2019/12/03)
The ability of G protein-coupled receptor (GPCR) kinases (GRKs) to regulate desensitization of GPCRs has made GRK2 and GRK5 attractive targets for treating heart failure and other diseases such as cancer. Although advances have been made toward developing inhibitors that are selective for GRK2, there have been far fewer reports of GRK5 selective compounds. Herein, we describe the development of GRK5 subfamily selective inhibitors, 5 and 16d that covalently interact with a nonconserved cysteine (Cys474) unique to this subfamily. Compounds 5 and 16d feature a highly amenable pyrrolopyrimidine scaffold that affords high nanomolar to low micromolar activity that can be easily modified with Michael acceptors with various reactivities and geometries. Our work thereby establishes a new pathway toward further development of subfamily selective GRK inhibitors and establishes Cys474 as a new and useful covalent handle in GRK5 drug discovery.
