Novel Thiazole-Fused [4,5-g] or [5,4-g]Quinazolin-8-ones and Their Quinazoline Analogues: Synthesis and Biological Evaluation

Autor: Nathan Broudic, Alexandra Pacheco-Benichou, Cécile Corbière, Blandine Baratte, Thomas Robert, Stéphane Bach, Hélène Solhi, Rémy Le Guével, Corinne Fruit, Thierry Besson

Publikováno v: Pharmaceuticals, Vol 17, Iss 11, p 1452 (2024)

Background/Objectives: In connection with previous work on V-shaped polycyclic thiazolo[5,4-f]quinazolin-9-one and [5,4-f]quinazoline derivatives that can modulate the activity of various kinases, the synthesis of straight thiazole-fused [4,5-g] or [

Externí odkaz: https://doaj.org/article/9fca41b7c93b4c3b930e5e47bdadcea3

Synthesis of 2-Cyanobenzothiazoles via Pd-Catalyzed/Cu-Assisted C-H Functionalization/Intramolecular C-S Bond Formation from N-Arylcyanothioformamides

Autor: Nathan Broudic, Alexandra Pacheco-Benichou, Corinne Fruit, Thierry Besson

Publikováno v: Molecules, Vol 27, Iss 23, p 8426 (2022)

We report herein on a catalytic system involving palladium and copper to achieve the cyclization of N-arylcyanothioformamides and the synthesis of 2-cyanobenzothiazoles. The C-H functionalization/intramolecular C-S bond formation reaction was achieve

Externí odkaz: https://doaj.org/article/8e55cd5631bb4dc2a1da8e63f66affed

Microwave-assisted copper catalyzed C-H arylation of bioactive pyrimidinones using diaryliodoniums salts

Autor: Corinne Fruit, Thierry Besson, Alexandra Pacheco-Benichou

Publikováno v: Proceedings of 7th International Electronic Conference on Medicinal Chemistry.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f1bfa5b00d46e2e7f0854bebf275d1b1
https://doi.org/10.3390/ecmc2021-11583

DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STAT3

Autor: Malini Rammohan, Nobuko Hijiya, Sébastien Malinge, Shai Izraeli, Praveen Suraneni, Young Ah Goo, Beat Bornhauser, Qiang Wen, Anouchka P. Laurent, Thierry Besson, Benjamin J. Thompson, Jean-Pierre Bourquin, Rahul S. Bhansali, Corinne Fruit, Ethan James Harris, Yi Chien Tsai, John D. Crispino, Maria Vilenchik, Paul Lee, Aurelie Siret, Bon Ham Yip, Alexandra Pacheco-Benichou, Silvia Jenni

Publikováno v: J Clin Invest
Journal of Clinical Investigation
Journal of Clinical Investigation, American Society for Clinical Investigation, 2021, 131 (1), ⟨10.1172/JCI135937⟩

DYRK1A is a serine/threonine kinase encoded on human chromosome 21 (HSA21) that has been implicated in several pathologies of Down syndrome (DS), including cognitive deficits and Alzheimer's disease. Although children with DS are predisposed to devel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f2a5f8992bfcfc1504bfe94b23253134
https://europepmc.org/articles/PMC7773384/

Diaryliodoniums Salts as Coupling Partners for Transition-Metal Catalyzed C- and N-Arylation of Heteroarenes

Autor: Corinne Fruit, Alexandra Pacheco-Benichou, Thierry Besson

Publikováno v: Catalysts
Catalysts, MDPI, 2020, 10 (5), pp.483. ⟨10.3390/catal10050483⟩
Catalysts, Vol 10, Iss 483, p 483 (2020)

International audience; Owing to the pioneering works performed on the metal-catalyzed sp2 C–H arylation of indole and pyrrole by Sanford and Gaunt, N– and C-arylation involving diaryliodonium salts offers an attractive complementary strategy for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5d552f25bfd04cbbcf8e207d8c4b51b
https://hal-normandie-univ.archives-ouvertes.fr/hal-02557380