Multiparameter Optimization of Oxidative Phosphorylation Inhibitors for the Treatment of Pancreatic Cancer.
Adenosine Triphosphate
/ biosynthesis
Animals
Antineoplastic Agents
/ chemical synthesis
Cell Line, Tumor
Drug Discovery
Drug Screening Assays, Antitumor
Female
Humans
Mice
Mice, Inbred C57BL
NAD
/ metabolism
Oxidative Phosphorylation
/ drug effects
Pancreatic Neoplasms
/ drug therapy
Sulfonamides
/ chemical synthesis
Xenograft Model Antitumor Assays
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
24 02 2022
24 02 2022
Historique:
pubmed:
16
2
2022
medline:
11
3
2022
entrez:
15
2
2022
Statut:
ppublish
Résumé
Targeting oxidative phosphorylation (OXPHOS) complexes is an emerging strategy to disrupt the metabolism of select cancer subtypes and to overcome resistance to targeted therapies. Here, we describe our lead optimization campaign on a series of benzene-1,4-disulfonamides as novel OXPHOS complex I inhibitors. This effort led to the discovery of compound
Identifiants
pubmed: 35167303
doi: 10.1021/acs.jmedchem.1c01934
pmc: PMC9165018
mid: NIHMS1811429
doi:
Substances chimiques
Antineoplastic Agents
0
Sulfonamides
0
NAD
0U46U6E8UK
Adenosine Triphosphate
8L70Q75FXE
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
3404-3419Subventions
Organisme : NCI NIH HHS
ID : R01 CA188252
Pays : United States
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