Cytotoxic 1,2,3-Triazoles as Potential Leads Targeting the S100A2-p53 Complex: Synthesis and Cytotoxicity.
Antineoplastic Agents
/ chemical synthesis
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Chemotactic Factors
/ antagonists & inhibitors
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Docking Simulation
Molecular Structure
S100 Proteins
/ antagonists & inhibitors
Structure-Activity Relationship
Triazoles
/ chemical synthesis
Tumor Cells, Cultured
Tumor Suppressor Protein p53
/ antagonists & inhibitors
S100A2
drug design
focused library
p53
pancreatic cancer
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
16 09 2021
16 09 2021
Historique:
revised:
18
05
2021
received:
09
12
2020
pubmed:
29
5
2021
medline:
17
2
2022
entrez:
28
5
2021
Statut:
ppublish
Résumé
In silico screening predicted 1 (N-(4-((4-(3-(4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl)propyl)piperazin-1-yl) sulfonyl)-phenyl)acetamide) as an inhibitor of the S100A2-p53 protein-protein interaction. S100A2 is a validated pancreatic cancer drug target. In the MiaPaCa-2 pancreatic cell line, 1 was a ∼50 μM growth inhibitor. Synthesis of five focused compound libraries and cytotoxicity screening revealed increased activity from the presence of electron withdrawing moieties on the sulfonamide aromatic ring, with the 3,5-bis-CF
Identifiants
pubmed: 34047450
doi: 10.1002/cmdc.202000950
doi:
Substances chimiques
Antineoplastic Agents
0
Chemotactic Factors
0
S100 Proteins
0
S100A2 protein, human
0
Triazoles
0
Tumor Suppressor Protein p53
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
2864-2881Subventions
Organisme : UON UPRS and Binzhou Medical University (China)
Informations de copyright
© 2021 Wiley-VCH GmbH.
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