Results 1 to 10 of about 29 (29)

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

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

Etude de la fonctionnalisation de thiazolo[5,4-f]quinazolin-9(8H)-ones via des sel de diaryliodonium et synthèse de nouvelles thiazolo[4,5-g]quinazolin-8(7H)-ones, potentiels inhibiteurs de kinases.

La synthèse de structures polyhétérocycliques aromatiques est étudiée par notre groupe depuis plus de vingt ans. La modulation fonctionnelle de ces noyaux a conduit à deux composés de référence, inhibiteurs de la kinase DYRK1A : EHT1610 et FC162. Afin de comprendre l’implication de cette kinase dans des maladies neurodégénératives comme la maladie d ...
openaire   +1 more source

Photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones

Chinese Journal of Catalysis, 2021
Bing Yu, Kai Sun, Fang Xiao
exaly  

Visible-light-induced three-component reaction of quinoxalin-2(1H)-ones, alkenes and CF3SO2Na leading to 3-trifluoroalkylated quinoxalin-2(1H)-ones

Chinese Chemical Letters, 2021
Xiaohui Zhao, Wei Wei, Yufen Lv
exaly  

C(sp2)–H/O–H cross-dehydrogenative coupling of quinoxalin-2(1H)-ones with alcohols under visible-light photoredox catalysis

Chinese Journal of Catalysis, 2020
Zhong Cao, Wei-Min He, Long-Yong Xie
exaly