Identification of novel 2-(1H-indol-1-yl)-benzohydrazides CXCR4 ligands impairing breast cancer growth and motility
| العنوان: | Identification of novel 2-(1H-indol-1-yl)-benzohydrazides CXCR4 ligands impairing breast cancer growth and motility |
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| المؤلفون: | Vircillo Valentina, Badolato Mariateresa, Giordano Cinzia, Ando Sebastiano, Chemi Francesca, Aiello Francesca, Catalano Stefania, Barone Ines, Michela Cancellieri, Andrea Brancale, Garofalo Antonio, Bonofiglio Daniela, Grande Fedora |
| المصدر: | Future Medicinal Chemistry. 8:93-106 |
| بيانات النشر: | Future Science Ltd, 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | 0301 basic medicine, Receptors, CXCR4, RM, Motility, Antineoplastic Agents, Breast Neoplasms, Pharmacology, Biology, Ligands, CXCR4, RC0254, 03 medical and health sciences, 0302 clinical medicine, Breast cancer, Cell Movement, Catalytic Domain, Cell Line, Tumor, Drug Discovery, medicine, Humans, Receptor, Cell Proliferation, Tumor microenvironment, Binding Sites, Ligand, medicine.disease, Chemokine CXCL12, Molecular Docking Simulation, Hydrazines, 030104 developmental biology, Drug Design, 030220 oncology & carcinogenesis, Cancer research, Molecular Medicine, Female, Breast cancer cells, Whole cell, Signal Transduction |
| الوصف: | Background: Stromal-derived-factor-1 (SDF-1) and the G-protein-coupled receptor CXCR4 are involved in several physiological and pathological processes including breast cancer spread and progression. Several CXCR4 antagonists have currently reached advanced development stages as potential therapeutic agents for different diseases. Results: A small series of novel CXCR4 ligands, based on a 2-(1H-indol-1-yl)-benzohydrazide scaffold, has been designed and synthesized. The interaction with CXCR4-active site was predicted by molecular docking and confirmed by whole cell-based [125I]-SDF-1 ligand competition binding assays. One of the synthesized compounds was particularly active in blocking SDF-1-induced breast cancer cell motility, proliferation and downstream signaling activation in different breast cancer cell models and coculture systems. Conclusion: The newly synthesized compounds represent suitable leads for the development of innovative therapeutic agents targeting CXCR4. |
| وصف الملف: | application/pdf |
| تدمد: | 1756-8927 1756-8919 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26b95062ab5af4291f7bd7e90ad1fe3f https://doi.org/10.4155/fmc.15.176 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....26b95062ab5af4291f7bd7e90ad1fe3f |
| قاعدة البيانات: | OpenAIRE |
PDF full text from Publisher | تدمد: | 17568927 17568919 |
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