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Your search keyword '"Béatrice Josselin"' showing total 2 results
Start Over Author "Béatrice Josselin" Journal bioorganic & medicinal chemistry
2 results on '"Béatrice Josselin"'

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

Author

Béatrice Josselin, Yannick J. Esvan, Fabrice Anizon, Wael Zeinyeh, Vincent Théry, Blandine Baratte, Lionel Nauton, Stéphane Bach, Pascale Moreau, Sandrine Ruchaud, Francis Giraud, Institut de Chimie de Clermont-Ferrand (ICCF), SIGMA Clermont (SIGMA Clermont)-Institut de Chimie du CNRS (INC)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020])-Centre National de la Recherche Scientifique (CNRS), Station biologique de Roscoff (SBR), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS), Plate-forme de criblage d'inhibiteurs de protéines kinases=Kinase Inhibitor Specialized Screening facility (KISSf), Fédération de recherche de Roscoff (FR2424), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Station biologique de Roscoff (SBR), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Biologie Intégrative (LBI), Commissariat à l'énergie atomique et aux énergies alternatives (CEA), Laboratoire de Biologie Intégrative des Modèles Marins (LBI2M), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Station biologique de Roscoff (SBR), and Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)

Subjects
Molecular model, Pyridines, Stereochemistry, [SDV]Life Sciences [q-bio], Clinical Biochemistry, Pharmaceutical Science, Protein Serine-Threonine Kinases, 01 natural sciences, Biochemistry, CLK1, Glycogen Synthase Kinase 3, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Quinazoline, [CHIM]Chemical Sciences, Humans, Potency, [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology, Protein kinase A, Protein Kinase Inhibitors, Molecular Biology, ComputingMilieux_MISCELLANEOUS, [CHIM.ORGA]Chemical Sciences/Organic chemistry, 010405 organic chemistry, Kinase, Cyclin-dependent kinase 5, Organic Chemistry, Cyclin-Dependent Kinase 5, Protein-Tyrosine Kinases, Protein Structure, Tertiary, 3. Good health, 0104 chemical sciences, Molecular Docking Simulation, 010404 medicinal & biomolecular chemistry, chemistry, Quinazolines, Molecular Medicine, Casein kinase 1, Protein Kinases
Abstract

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 its potency against the same protein kinase panel was compared to the analogous pyrido[3,4-g]quinazoline. Best results were obtained for 10-nitropyrido[3,4-g]quinazoline 4 toward CLK1 with nanomolar activities.

Published
2019
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2. Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors

Author

Lesetja J. Legoabe, Stéphane Bach, Malikotsi A. Qhobosheane, Sandrine Ruchaud, Béatrice Josselin, Richard M. Beteck, Jacobus P. Petzer, Laboratoire de Biologie Intégrative des Modèles Marins (LBI2M), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Station biologique de Roscoff (SBR), Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), 10727388 - Petzer, Jacobus Petrus, 12902608 - Legoabe, Lesetja Jan, 25159194 - Beteck, Richard Mbi, and 27836576 - Qhobosheane, Malikotsi A.

Subjects
Benzocycloalkanone, Indoles, 7-Azaindole, [SDV]Life Sciences [q-bio], Clinical Biochemistry, Pharmaceutical Science, Protein Serine-Threonine Kinases, 01 natural sciences, Biochemistry, Protein kinase, Structure-Activity Relationship, CDK9/CyclinT, Drug Discovery, Humans, [CHIM]Chemical Sciences, Structure–activity relationship, Protein kinase A, Protein Kinase Inhibitors, Molecular Biology, ComputingMilieux_MISCELLANEOUS, Biological evaluation, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Kinase, Chemistry, Haspin, Organic Chemistry, Intracellular Signaling Peptides and Proteins, Dual inhibitor, Ketones, Structure-activity relationship, Cyclin-Dependent Kinase 9, 3. Good health, 0104 chemical sciences, Molecular Docking Simulation, 010404 medicinal & biomolecular chemistry, Oncology, Molecular Medicine, Cyclin-dependent kinase 9
Abstract

Protein kinases are important drug targets, especially in the area of oncology. This paper reports the synthesis and biological evaluation of new 7-azaindole derivatives bearing benzocycloalkanone motifs as potential protein kinase inhibitors. Four compounds 8g, 8h, 8i, and 8l were discovered to inhibit cyclin-dependent kinase 9 (CDK9/CyclinT) and/or Haspin kinase in the micromolar to nanomolar range. 8l was identified as the most potent Haspin inhibitor (IC50 = 14 nM), while 8g and 8h acted as dual inhibitors of CDK9/CyclinT and Haspin. These novel compounds constitute a promising starting point for the discovery of dual protein kinase inhibitors that have potential to be developed as anticancer agents, since both CDK9/CyclinT and Haspin are considered to be drug targets in oncology.

Published
2020
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