Synthesis of novel 5-substituted indirubins as protein kinases inhibitors

Autor: Anne Beauchard, Olivier Lozach, Thierry Besson, Laurent Meijer, Mélina Blairvacq, Valérie Thiéry, Yoan Ferandin, Stéphane Frère
Přispěvatelé: Institut national de recherches archéologiques préventives (Inrap), Mer et santé (MS), Station biologique de Roscoff [Roscoff] (SBR), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS), Molécules et cibles thérapeutiques (MCT), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Génie Protéique et Cellulaire (LGPC), Université de La Rochelle (ULR), La Rochelle Université (ULR), Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)
Rok vydání: 2006
Předmět:
Indoles
Swine
Clinical Biochemistry
Cyclin B
Pharmaceutical Science
[CHIM.THER]Chemical Sciences/Medicinal Chemistry
01 natural sciences
Biochemistry
Glycogen Synthase Kinase 3
Starfish
chemistry.chemical_compound
MESH: Structure-Activity Relationship
Drug Discovery
CDC2-CDC28 Kinases
MESH: Protein Kinase Inhibitors
MESH: Animals
MESH: Swine
ComputingMilieux_MISCELLANEOUS
MESH: Glycogen Synthase Kinase 3
MESH: Indoles
MESH: Starfish
Molecular Structure
biology
[CHIM.ORGA]Chemical Sciences/Organic chemistry
Kinase
MESH: Molecular Weight
Stereoisomerism
3. Good health
MESH: Cell Survival
Enzyme inhibitor
Molecular Medicine
MESH: Cell Line
Tumor

Cell Survival
MESH: Molecular Structure
010402 general chemistry
Structure-Activity Relationship
[CHIM.ANAL]Chemical Sciences/Analytical chemistry
Cyclin-dependent kinase
Cell Line
Tumor

Animals
Humans
Structure–activity relationship
[SDV.BBM]Life Sciences [q-bio]/Biochemistry
Molecular Biology

Protein kinase A
MESH: CDC2-CDC28 Kinases
Protein Kinase Inhibitors
Molecular Biology
Cyclin-dependent kinase 1
MESH: Humans
010405 organic chemistry
Organic Chemistry
[CHIM.CATA]Chemical Sciences/Catalysis
MESH: Stereoisomerism
0104 chemical sciences
Molecular Weight
chemistry
biology.protein
Indirubin
Zdroj: Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry, 2006, 14 (18), pp.6434-43. ⟨10.1016/j.bmc.2006.05.036⟩
Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2006, 14 (18), pp.6434-6443. ⟨10.1016/j.bmc.2006.05.036⟩
Bioorganic and Medicinal Chemistry Letters, 2006, 14 (18), pp.6434-6443. ⟨10.1016/j.bmc.2006.05.036⟩
Bioorganic and Medicinal Chemistry, Elsevier, 2006, 14 (18), pp.6434-43. ⟨10.1016/j.bmc.2006.05.036⟩
ISSN: 0968-0896
1464-3391
0960-894X
DOI: 10.1016/j.bmc.2006.05.036
Popis: In an effort to identify new pharmacological inhibitors of disease-relevant protein kinases with increased potency and selectivity, we synthesized and evaluated new 5-substituted indirubins. The effects of 34 indirubin derivatives on CDK1/cyclin B, CDK5/p25, and GSK-3, as well as on SH-SY5Y human neuroblastoma cell survival, were investigated.
Databáze: OpenAIRE