Design and Synthesis of Novel 2-Acetamido, 6-Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors - In vitro Evaluation of their Antiproliferative Activity.
BRAFV600E inhibitors
Benzothiazole
Cancer
In silico studies
In vitro biological evaluation
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
16 Nov 2023
16 Nov 2023
Historique:
revised:
02
10
2023
received:
23
06
2023
medline:
29
11
2023
pubmed:
4
10
2023
entrez:
4
10
2023
Statut:
ppublish
Résumé
The oncogenic BRAFV600E kinase leads to abnormal activation of the MAPK signaling pathway and thus, uncontrolled cellular proliferation and cancer development. Based on our previous virtual screening studies which issued 2-acetamido-1,3 benzothiazole-6-carboxamide scaffold as active pharmacophore displaying selectivity against the mutated BRAF, eleven new substituted benzothiazole derivatives were designed and synthesized by coupling of 2-acetamidobenzo[d]thiazole-6-carboxylic acid with the appropriate amines in an effort to provide even more efficient inhibitors and tackle drug resistance often developed during cancer treatment. All derived compounds bore the benzothiazole scaffold substituted at position-2 by an acetamido moiety and at position-6 by a carboxamide functionality, the NH moiety of which was further linked through an alkylene linker to a sulfonamido (or amino) aryl (or alkyl) functionality or a phenylene linker to a sulfonamido aromatic (or non-aromatic) terminal pharmacophore in the order -C
Identifiants
pubmed: 37792577
doi: 10.1002/cmdc.202300322
doi:
Substances chimiques
Benzothiazoles
0
Antineoplastic Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
e202300322Subventions
Organisme : NSRF
ID : MIS 5002398
Organisme : Greece
Organisme : EU
Organisme : European Union
ID : MIS-5000432
Organisme : State Scholarships Foundation (ΙΚY)
Organisme : Infrastructure for Preclinical and early-Phase Clinical Development of Drugs, Therapeutics and Biomedical Devices (EATRIS-GR)
ID : MIS 5028091
Organisme : European Union
Informations de copyright
© 2023 The Authors. ChemMedChem published by Wiley-VCH GmbH.
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