ArticleACS medicinal chemistry letters2013
Discovery of tetrahydroisoquinoline-based CXCR4 antagonists.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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Who cites it
21 citing papers in PubMed.
- CXCR4-targeted PET imaging of glioblastoma using [EJNMMI radiopharmacy and chemistry · 2026Article
- Discovery of Novel 2-Morpholine Tetrahydroisoquinoline CXCR4 Antagonists with Unique Properties.Journal of medicinal chemistry · 2026Article
- Optimization of next-generation CXCR4 ligands for radiotheranostic applications.Frontiers in pharmacology · 2026Review
- Targeting the CXCR4/CXCL12 Axis in Cancer Therapy: Analysis of Recent Advances in the Development of Potential Anticancer Agents.Molecules (Basel, Switzerland) · 2025Review
- Radiosynthesis and preclinical evaluation of aEJNMMI radiopharmacy and chemistry · 2024Article
- Characterization of a CXCR4 antagonist TIQ-15 with dual tropic HIV entry inhibition properties.PLoS pathogens · 2024Article
- Light-Driven Enantioselective Carbene-Catalyzed Radical-Radical Coupling.Angewandte Chemie (International ed. in English) · 2023Article
- Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists.Molecules (Basel, Switzerland) · 2021Article
- Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings.ACS medicinal chemistry letters · 2021Article
- At the Bench: Pre-clinical evidence for multiple functions of CXCR4 in cancer.Journal of leukocyte biology · 2021Review
- Synthetic Activators of Cell Migration Designed by Constructive Machine Learning.ChemistryOpen · 2019Article
- Characterization, Dynamics, and Mechanism of CXCR4 Antagonists on a Constitutively Active Mutant.Cell chemical biology · 2019Article
- Tetrahydroisoquinoline CXCR4 Antagonists Adopt a Hybrid Binding Mode within the Peptide Subpocket of the CXCR4 Receptor.ACS medicinal chemistry letters · 2019Article
- Improving the inhibitory effect of CXCR4 peptide antagonist in tumor metastasis with an acetylated PAMAM dendrimer.RSC advances · 2018Article
- Discovery ofACS medicinal chemistry letters · 2018Article
- Small molecule CXCR4 antagonists block the HIV-1 Nef/CXCR4 axis and selectively initiate the apoptotic program in breast cancer cells.Oncotarget · 2018Article
- Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.ACS medicinal chemistry letters · 2018Article
- Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists.ACS medicinal chemistry letters · 2018Article
- Discovery of novel N-aryl piperazine CXCR4 antagonists.Bioorganic & medicinal chemistry letters · 2015Article
- Anti-HIV small-molecule binding in the peptide subpocket of the CXCR4:CVX15 crystal structure.Chembiochem : a European journal of chemical biology · 2014Article
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
A de novo hit-to-lead effort involving the redesign of benzimidazole-containing antagonists of the CXCR4 receptor resulted in the discovery of a novel series of 1,2,3,4-tetrahydroisoquinoline (TIQ) analogues. In general, this series of compounds show good potencies (3-650 nM) in assays involving CXCR4 function, including both inhibition of attachment of X4 HIV-1IIIB virus in MAGI-CCR5/CXCR4 cells and inhibition of calcium release in Chem-1 cells. Series profiling permitted the identification of TIQ-(R)-stereoisomer 15 as a potent and selective CXCR4 antagonist lead candidate with a promising in vitro profile. The drug-like properties of 15 were determined in ADME in vitro studies, revealing low metabolic liability potential. Further in vivo evaluations included pharmacokinetic experiments in rats and mice, where 15 was shown to have oral bioavailability (F = 63%) and resulted in the mobilization of white blood cells (WBCs) in a dose-dependent manner.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.