Results 1 to 10 of about 31 (31)

Metal-Free Visible-Light-Induced C–H/C–H Cross-Dehydrogenative-Coupling of Quinoxalin-2(H)-Ones With Simple Ethers

ACS Sustainable Chemistry and Engineering, 2018
Wei Wei, Daoshan Yang, Hua Wang
exaly  

The Chemistry and Biological Potential of Azetidin-2-Ones

European Journal of Medicinal Chemistry, 2014
Jaya Dwivedi, Kishor S Jain
exaly  

Synthesis of Thiazolo[5,4-f]quinazolin-9(8H)-ones as Multi-Target Directed Ligands of Ser/Thr Kinases [PDF]

Molecules, 2016
A library of thirty novel thiazolo[5,4-f]quinazolin-9(8H)-one derivatives belonging to four series designated as 12, 13, 14 and 15 was efficiently prepared, helped by microwave-assisted technology when required. The efficient multistep synthesis of methyl 6-amino-2-cyano- benzo[d]thiazole-7-carboxylate (1) has been reinvestigated and performed on a ...
Hédou, Damien, Godeau, Julien, Loaëc, N., Meijer, L., Fruit, Corinne, Besson, Thierry   +5 more
openaire   +5 more sources

Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A [PDF]

Pharmaceuticals, 2019
Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) hyperactivity has been linked to the development of a number of human malignancies. DYRK1A is the most studied family member, and the discovery of novel specific inhibitors is attracting considerable interest.
Corinne Fruit, Florence Couly, Rahul Bhansali, Malini Rammohan, Mattias F. Lindberg, John D. Crispino, Laurent Meijer, Thierry Besson   +7 more
openaire   +3 more sources

<strong>Late-stage C-H Arylation of Thiazolo[5,4-f]quinazolin-9(8H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors</strong> [PDF]

Proceedings of 3rd International Electronic Conference on Medicinal Chemistry, 2017
Thierry Besson, Florence Couly, Carole Dubouilh-benard, Laurent Meijer, Corinne Fruit   +4 more
openaire   +1 more source

Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. [PDF]

J Med Chem, 2020
Kang D, Ruiz FX, Feng D, Pilch A, Zhao T, Wei F, Wang Z, Sun Y, Fang Z, De Clercq E, Pannecouque C, Arnold E, Liu X, Zhan P.   +13 more
europepmc   +1 more source

Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. [PDF]

ACS Med Chem Lett, 2013
Guillon R, Pagniez F, Picot C, Hédou D, Tonnerre A, Chosson E, Duflos M, Besson T, Logé C, Le Pape P.   +9 more
europepmc   +1 more source

Late-Stage C–H Arylation of Thiazolo[5,4-f]quinazolin-9(8H)-one Backbone: Synthesis of an Array of Potential Kinase Inhibitors

Synthesis, 2017
Driven by the need of structural modification to establish structure-activity relationships, the regioselective C–H bond activation of thiazolo[5,4-f]quinazolin-9(8H)-one backbone has been developed to furnish the corresponding C2-arylated valuable scaffold.
Couly, Florence, Dubouilh-Benard, Carole, Besson, Thierry, Fruit, Corinne   +3 more
openaire   +2 more sources

ChemInform Abstract: Pd‐Catalyzed and Copper Assisted Regioselective Sequential C2 and C7 Arylation of Thiazolo[5,4‐f]quinazolin‐9(8H)‐one with Aryl Halides.

ChemInform, 2016
AbstractThe synthetically useful title transformation is performed in a convenient one‐pot manner.
Marine Harari, Florence Couly, Corinne Fruit, Thierry Besson   +3 more
openaire   +1 more source

Pd-Catalyzed and Copper Assisted Regioselective Sequential C2 and C7 Arylation of Thiazolo[5,4-f]quinazolin-9(8H)-one with Aryl Halides

Organic Letters, 2016
A selective functionalization of thiazolo[5,4-f]quinazolin-9(8H)-one has been developed through sequential activation of C-H bonds to furnish diarylated compounds. This strategy allows the regioselective C2 and C7 arylation by a judicious choice of coupling partners and bases, requiring no additional ligands or directing groups. Differently substituted
Harari, Marine, Couly, Florence, Fruit, Corinne, Besson, Thierry   +3 more
openaire   +4 more sources