ArticleJournal of medicinal chemistry2010
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 59 citations in OpenAlex.
- Conversion of all polyester units to amines: Ruthenium-catalyzed, acid-assisted hydrogenative amination.Science advances · 2026Article
- Anti-myeloma activity of the CXCR4 antagonist WZ811.Journal of molecular medicine (Berlin, Germany) · 2026Article
- Benzimidazol-2-ylidene ruthenium complexes for C-N bond formation through alcohol dehydrogenation.Turkish journal of chemistry · 2023Article
- Present status and future trends in molecular imaging of lymphocytes.Seminars in nuclear medicine · 2023Review
- Discovery of novel aminopiperidinyl amide CXCR4 modulators through virtual screening and rational drug design.European journal of medicinal chemistry · 2020Article
- Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure-Activity Relationship Studies, and Biological Assessment.ACS omega · 2020Article
- Mouse models of uveal melanoma: Strengths, weaknesses, and future directions.Pigment cell & melanoma research · 2020Review
- Development of CXCR4 modulators based on the lead compound RB-108.European journal of medicinal chemistry · 2019Article
- Targeting CXCL12/CXCR4 Axis in Tumor Immunotherapy.Current medicinal chemistry · 2019Review
- HDAC9 overexpression confers invasive and angiogenic potential to triple negative breast cancer cells via modulating microRNA-206.Biochemical and biophysical research communications · 2018Article
- Anti-inflammatory hybrids of secondary amines and amide-sulfamide derivatives.European journal of medicinal chemistry · 2018Article
- Novel anti-inflammatory agents targeting CXCR4: Design, synthesis, biological evaluation and preliminary pharmacokinetic study.European journal of medicinal chemistry · 2017Article
- Development of CXCR4 modulators by virtual HTS of a novel amide-sulfamide compound library.European journal of medicinal chemistry · 2017Article
- Synthesis and evaluation of an (18)F-labeled pyrimidine-pyridine amine for targeting CXCR4 receptors in gliomas.Nuclear medicine and biology · 2016Article
- Symmetrical bis-tertiary amines as novel CXCR4 inhibitors.European journal of medicinal chemistry · 2016Article
- Process of hepatic metastasis from pancreatic cancer: biology with clinical significance.Journal of cancer research and clinical oncology · 2016Review
- Synthesis of pyridine derivatives as potential antagonists of chemokine receptor type 4.Heterocyclic communications · 2014Article
- Expression of CXCL10 is associated with response to radiotherapy and overall survival in squamous cell carcinoma of the tongue.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2014Article
- High-level expression of CXCR4 in breast cancer is associated with early distant and bone metastases.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2014Article
- Inhibition of angiogenesis, fibrosis and thrombosis by tetramethylpyrazine: mechanisms contributing to the SDF-1/CXCR4 axis.PloS one · 2014Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
The C-X-C chemokine receptor type 4 (CXCR4)/stromal cell derived factor-1 (SDF-1 or CXCL12) interaction and the resulting cell signaling cascade play a key role in metastasis and inflammation. On the basis of the previously published CXCR4 antagonist 5 (WZ811), a series of novel nonpeptidic anti-CXCR4 small molecules have been designed and synthesized to improve potency. Following a structure-activity profile around 5, more advanced compounds in the N,N'-(1, 4-phenylenebis(methylene)) dipyrimidin-2-amines series were discovered and shown to possess higher CXCR4 binding potential and specificity than 5. Compound 26 (508MCl) is the lead compound and exhibits subnanomolar potency in three in vitro assays including competitive binding, Matrigel invasion and Gα(i) cyclic adenosine monophosphate (cAMP) modulation signaling. Furthermore, compound 26 displays promising effects by interfering with CXCR4 function in three mouse models: paw inflammation, Matrigel plug angiogenesis, and uveal melanoma micrometastasis. These data demonstrate that dipyrimidine amines are unique CXCR4 antagonists with high potency and specificity.
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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.