Pharmacophore-based small molecule CXCR4 ligands

SAR studies of low molecular weight CXCR4 ligands are reported. Low molecular weight CXCR4 ligands were developed based on the peptide T140, which has previously been identified as a potent CXCR4 antagonist. Some compounds with naphthyl, fluorobenzyl and pyridyl moieties as pharmacophore groups in t...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-06, Vol.22 (12), p.4169-4172
Main Authors: Narumi, Tetsuo, Tanaka, Tomohiro, Hashimoto, Chie, Nomura, Wataru, Aikawa, Haruo, Sohma, Akira, Itotani, Kyoko, Kawamata, Miyako, Murakami, Tsutomu, Yamamoto, Naoki, Tamamura, Hirokazu
Format: Article
Language:English
Subjects:
AIDS
antagonists
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
antiretroviral agents
Antiviral activity
Antiviral agents
Biological and medical sciences
Cell Line
Chemokine receptor
HIV entry inhibitors
HIV-1 - drug effects
HIV-1 - physiology
Human immunodeficiency virus
Humans
Ligands
Low molecular weight CXCR4 ligands
Medical sciences
molecular weight
Oligopeptides - chemical synthesis
Oligopeptides - chemistry
Oligopeptides - pharmacology
pharmacology
Pharmacology. Drug treatments
Receptors, CXCR4 - antagonists & inhibitors
Receptors, CXCR4 - chemistry
Small Molecule Libraries
Structure-Activity Relationship
structure-activity relationships
T-Lymphocytes - drug effects
T-Lymphocytes - virology
Virus Replication - drug effects
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Description
Summary:SAR studies of low molecular weight CXCR4 ligands are reported. Low molecular weight CXCR4 ligands were developed based on the peptide T140, which has previously been identified as a potent CXCR4 antagonist. Some compounds with naphthyl, fluorobenzyl and pyridyl moieties as pharmacophore groups in the molecule showed significant CXCR4-binding activity and anti-HIV activity. Structure–activity relationships were studied and characteristics of each of these three moieties necessary for CXCR4 binding were defined. In this way, CXCR4 ligands with two types of recognition modes for CXCR4 have been found.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.04.032