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Identification of novel 2-(1H-Indol-1-yl)benzohydrazides CXCR4 ligands impairing breast cancer growth and motility

Fedora, Grande, Ines, Barone, Francesca, Aiello, Brancale, Andrea ORCID:, Cancellieri, Michela, Mariateresa, Badolato, Francesca, Chemi, Cinzia, Giordano, Valentina, Vircillo, Daniela, Bonofiglio, Antonio, Garofalo, Sebastiano, Ando and Stefania, Catalano 2016. Identification of novel 2-(1H-Indol-1-yl)benzohydrazides CXCR4 ligands impairing breast cancer growth and motility. Future Medicinal Chemistry 8 (2) , pp. 93-106. 10.4155/fmc.15.176

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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

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
R Medicine > RM Therapeutics. Pharmacology
Additional Information: Published online: 25 January 2016 Pdf uploaded in accordance with publisher's policy at (accessed 14/03/2016)
Publisher: Future Science
ISSN: 1756-8919
Date of First Compliant Deposit: 30 March 2016
Date of Acceptance: 17 November 2015
Last Modified: 07 Nov 2023 04:45

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