Synthesis and Kinase Inhibitory Potencies of Pyrazolo[3,4-g]isoquinolines

Autor: Mathilde Defois, Chloé Rémondin, Béatrice Josselin, Lionel Nauton, Vincent Théry, Fabrice Anizon, Sandrine Ruchaud, Francis Giraud, Pascale Moreau

Publikováno v: Molecules, Vol 27, Iss 17, p 5578 (2022)

A new series of pyrazolo[3,4-g]isoquinoline derivatives, diversely substituted at the 4- or 8-position, were synthesized. The results of the kinase inhibitory potency study demonstrated that the introduction of a bromine atom at the 8-position was de

Externí odkaz: https://doaj.org/article/235ac25b2e844150b7176e85977cbef4

QM/MM Study of Human Transketolase: Thiamine Diphosphate Activation Mechanism and Complete Catalytic Cycle

Autor: Laurence Hecquet, Vincent Théry, Lionel Nauton

Publikováno v: Journal of Chemical Information and Modeling
Journal of Chemical Information and Modeling, American Chemical Society, 2021, ⟨10.1021/acs.jcim.1c00190⟩
Journal of Chemical Information and Modeling, 2021, ⟨10.1021/acs.jcim.1c00190⟩

International audience; A computational model for human transketolase was proposed, showing that thiamine diphosphate activation was based on His110 in place of His481 reported in yeast transketolase. In addition, a complete catalytic reaction pathwa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7df588d053c644a135ba0d688f021d5
https://pubmed.ncbi.nlm.nih.gov/34161071

Kinase inhibitions in pyrido[4,3-h] and [3,4-g]quinazolines: Synthesis, SAR and molecular modeling studies

Autor: Béatrice Josselin, Yannick J. Esvan, Fabrice Anizon, Wael Zeinyeh, Vincent Théry, Blandine Baratte, Lionel Nauton, Stéphane Bach, Pascale Moreau, Sandrine Ruchaud, Francis Giraud

Publikováno v: Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry, 2019, 27 (10), pp.2083-2089. ⟨10.1016/j.bmc.2019.04.005⟩
Bioorganic and Medicinal Chemistry, Elsevier, 2019, 27 (10), pp.2083-2089. ⟨10.1016/j.bmc.2019.04.005⟩

New pyrido[3,4-g]quinazoline derivatives were prepared and evaluated for their inhibitory potency toward 5 protein kinases (CLK1, DYRK1A, GSK3, CDK5, CK1). A related pyrido[4,3-h]quinazoline scaffold with an angular structure was also synthesized and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c29954f2df2b1c4a2e326312b880bcb
https://doi.org/10.1016/j.bmc.2019.04.005

Pyridin-2(1H)one derivatives: A possible new class of therapeutics for mechanical allodynia

Autor: Fabrice Anizon, Isabelle Abrunhosa-Thomas, Radhouane Dallel, Vincent Théry, Francis Giraud, Pascale Moreau, Lionel Nauton, Alexia Visseq, Nicolas Pinto-Pardo, Amélie Descheemaeker, Alain Artola

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2020, 187, pp.111917. ⟨10.1016/j.ejmech.2019.111917⟩
European Journal of Medicinal Chemistry, 2020, 187, pp.111917. ⟨10.1016/j.ejmech.2019.111917⟩

Mechanical Allodynia (MA), a frequent chronic pain symptom caused by innocuous stimuli, constitutes an unmet medical need, as treatments using analgesics available today are not always effective and can be associated with important side-effects. A se

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27c04f243c9e7b9f6c47116987869cd9
https://hal.archives-ouvertes.fr/hal-02444268

New N-1,N-10-bridged pyrrolo[2,3-a]carbazole-3-carbaldehydes: Synthesis and biological activities

Autor: Vincent Théry, Pascale Moreau, Stein Ove Døskeland, Fabrice Anizon, Francis Giraud, Lars Herfindal, Marion Bourhis, Lionel Nauton

Publikováno v: Bioorganic Chemistry
Bioorganic Chemistry, Elsevier, 2014, 57, pp.108-115. ⟨10.1016/j.bioorg.2014.09.004⟩
Bioorganic Chemistry, 2014, 57, pp.108-115. ⟨10.1016/j.bioorg.2014.09.004⟩

International audience; The synthesis of new pyrrolocarbazoles substituted at N-1/N-10 positions is described. All the compounds tested demonstrated moderate to high Pim-1/Pim-3 kinase inhibitory potency. The most active inhibitors identified in this

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4163058f2885e2580e630a878aa429bd
https://doi.org/10.1016/j.bioorg.2014.09.004