Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.

Humans Ligands Pyrazinamide Copper Pancreatic Neoplasms / drug therapy Receptors, sigma / metabolism Pancreatic Neoplasms

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:
09 02 2023
Historique:
pubmed: 25 1 2023
medline: 11 2 2023
entrez: 24 1 2023
Statut: ppublish

Résumé

Sigma 2 receptor (σ2R) is overexpressed in select cancers and is regarded as a biomarker for tumor proliferation. σ2R ligands are emerging as promising theranostics for cancer and neurodegenerative diseases. Herein, we describe the design and synthesis of a series of novel quinolyl pyrazinamides as selective and potent σ2R ligands that show sub-micromolar potency in pancreatic cancer cell lines. Compounds

Identifiants

DOI: 10.1021/acs.jmedchem.2c01769 PMID: 36692906
pubmed: 36692906
doi: 10.1021/acs.jmedchem.2c01769
doi:

Substances chimiques

Ligands 0
Pyrazinamide 2KNI5N06TI
Copper 789U1901C5
Receptors, sigma 0

Types de publication

Journal Article Research Support, N.I.H., Extramural

Langues

eng

Sous-ensembles de citation

IM

Pagination

1990-2019

Subventions

Organisme : NCI NIH HHS
ID : R01 CA272641
Pays : United States

Auteurs

Joyeeta Roy (J)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
ORCID: 0000-0002-4904-0551

Armita Kyani (A)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.

Maha Hanafi (M)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
ORCID: 0000-0002-5389-4656

Yibin Xu (Y)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
ORCID: 0000-0002-8261-3286

John Takyi-Williams (J)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
Pharmaceutical Sciences, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.

Duxin Sun (D)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
Pharmaceutical Sciences, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
ORCID: 0000-0002-6406-2126

Essam Eldin A Osman (EEA)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
ORCID: 0000-0002-0768-9862

Nouri Neamati (N)

Departments of Medicinal Chemistry, College of Pharmacy, Rogel Cancer Center, University of Michigan, North Campus Research Complex, 1600 Huron Parkway, Ann Arbor, Michigan 48109, United States.
ORCID: 0000-0003-3291-7131

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Design and Synthesis of Orally Active Quinolyl...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Design and Synthesis of Orally Active Quinolyl...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrazines › Pyrazinamide › Design and Synthesis of Orally Active Quinolyl...
questionsmedicales.fr › Produits chimiques inorganiques › Métaux › Métaux lourds › Cuivre › Design and Synthesis of Orally Active Quinolyl...
questionsmedicales.fr › Maladies endocriniennes › Tumeurs des glandes endocrines › Tumeurs du pancréas › Design and Synthesis of Orally Active Quinolyl...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteur aux neuropeptides › Récepteurs aux opioïdes › Récepteur sigma › Design and Synthesis of Orally Active Quinolyl...
questionsmedicales.fr › Maladies endocriniennes › Tumeurs des glandes endocrines › Tumeurs du pancréas › Design and Synthesis of Orally Active Quinolyl...