| Title: |
Synthesis, docking study and kinase inhibitory activity of a number of new substituted pyrazolo[3,4-c]pyridines |
| Authors: |
Sklepari, Meropi; Lougiakis, Nikolaos; Papastathopoulos, Athanasios; Pouli, Nicole; Marakos, Panagiotis; Myrianthopoulos, Vassilios; Robert, Thomas; Bach, Stéphane; Mikros, Emmanuel; Ruchaud, Sandrine |
| Contributors: |
Department of Pharmaceutical Chemistry; PharmaGnose S.A.; Station biologique de Roscoff = Roscoff Marine Station (SBR); Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS); Laboratoire de Biologie Intégrative des Modèles Marins (LBI2M); Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Station biologique de Roscoff = Roscoff Marine Station (SBR); Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-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 = Roscoff Marine Station (SBR); Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)-Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS) |
| Source: |
ISSN: 0009-2363. |
| Publisher Information: |
CCSD; Pharmaceutical Society of Japan |
| Publication Year: |
2017 |
| Subject Terms: |
pyrazolopyridine; kinase inhibition; GSK3α/β; purine analogues; molecular simulations; [SDV]Life Sciences [q-bio]; [CHIM]Chemical Sciences; [CHIM.ORGA]Chemical Sciences/Organic chemistry |
| Description: |
International audience ; A series of new pyrazolo[3,4-c]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against GSK3α/β as well as against CLK1 and DYRK1A, with good selectivity and remarkable SARs, without being cytotoxic. Molecular simulations in corelation with biological data revealed the importance of the existence of N1-H as well as the absence of a bulky 7-substituent. |
| Document Type: |
article in journal/newspaper |
| Language: |
English |
| DOI: |
10.1248/cpb.c16-00704 |
| Availability: |
https://hal.science/hal-03875290; https://hal.science/hal-03875290v1/document; https://hal.science/hal-03875290v1/file/42-Sklepari_et_al_Chem_Pharm_Bull.pdf; https://doi.org/10.1248/cpb.c16-00704 |
| Rights: |
https://about.hal.science/hal-authorisation-v1/ ; info:eu-repo/semantics/OpenAccess |
| Accession Number: |
edsbas.CB59C208 |
| Database: |
BASE |