Anticancer properties of bisaminoquinolines with modified linkers.
Aminoquinolines
/ chemical synthesis
Antineoplastic Agents
/ chemical synthesis
Autophagy
/ drug effects
Cell Line, Tumor
Drug Design
Drug Screening Assays, Antitumor
Enzyme Inhibitors
/ chemical synthesis
Humans
Hydrophobic and Hydrophilic Interactions
Membrane Proteins
/ antagonists & inhibitors
Molecular Structure
Thiolester Hydrolases
/ antagonists & inhibitors
Anticancer
Autophagy
Dimer
Quinoline
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 10 2021
01 10 2021
Historique:
received:
05
05
2021
revised:
28
06
2021
accepted:
14
07
2021
pubmed:
24
7
2021
medline:
28
12
2021
entrez:
23
7
2021
Statut:
ppublish
Résumé
We have previously reported the unique features of dimeric bisaminoquinolines as anticancer agents and have identified their cellular target as PPT1, a protein palmitoyl-thioesterase. We now report a systematic study on the role of the linker in these constructs, both with respect to the distance between the heterocycles, the linker hydrophobicity and the methylation status (primary vs. secondary vs. tertiary) of the central nitrogen atom on the observed biological activity.
Identifiants
pubmed: 34298133
pii: S0960-894X(21)00499-6
doi: 10.1016/j.bmcl.2021.128272
pmc: PMC8429239
mid: NIHMS1730730
pii:
doi:
Substances chimiques
Aminoquinolines
0
Antineoplastic Agents
0
Enzyme Inhibitors
0
Membrane Proteins
0
Thiolester Hydrolases
EC 3.1.2.-
PPT1 protein, human
EC 3.1.2.22
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
128272Subventions
Organisme : NCI NIH HHS
ID : P01 CA114046
Pays : United States
Organisme : NCI NIH HHS
ID : P30 CA016520
Pays : United States
Informations de copyright
Copyright © 2021 Elsevier Ltd. All rights reserved.
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