Straightforward synthesis of bis-tetraazacycloalkanes: towards new potential CXCR4 antagonists?

Nicolas Sok 1, * Isabelle Baglin 2 Christelle Basset 3 Fatima Fakkor 4 Evelyne Kohli 3 Yoann Rousselin 2 Claire Bernhard 2 Frédéric Boschetti 5 Christine Goze 2 Franck Denat 2, *
* Auteur correspondant
1 PAM - Procédés Alimentaires et Microbiologiques [Dijon]
2 ICMUB - Institut de Chimie Moléculaire de l'Université de Bourgogne [Dijon]
3 LNC - Lipides - Nutrition - Cancer [Dijon - U1231]
4 CHU Dijon - Centre Hospitalier Universitaire de Dijon - Hôpital François Mitterrand
5 CheMatech - Macrocycle Design Technologies
Abstract : We report herein an efficient and general method for the synthesis of new bismacrocyclic compounds, structural analogues of biscyclam AMD3100, in which the two macrocycles are linked together through carbon atoms of the cycles. Several representatives of this new class of biscyclic derivatives were prepared by reacting C-aminomethyl-13aneN4 with aromatic dialdehydes. Preliminary in vitro studies were performed to evaluate the affinity of these compounds towards the co-receptor CXCR4.
Keywords : Breast-cancer metastasis Chemokine receptor cxcr4 Inhibitors Amd3100 Complexes Discovery Story Hiv-1
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Article dans une revue
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https://hal-univ-bourgogne.archives-ouvertes.fr/hal-01560414
Contributeur : Pam - Université de Bourgogne <>
Soumis le : mardi 11 juillet 2017 - 15:25:58
Dernière modification le : jeudi 20 septembre 2018 - 16:35:40

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UNIV-BOURGOGNE | CNRS | LNC-UMR866 | INC-CNRS | PAM | ICMUB | AGROSUP-DIJON | AGROSUP-PAM | LNC-HSPPATHIES

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Nicolas Sok, Isabelle Baglin, Christelle Basset, Fatima Fakkor, Evelyne Kohli, et al.. Straightforward synthesis of bis-tetraazacycloalkanes: towards new potential CXCR4 antagonists?. RSC Advances, Royal Society of Chemistry, 2017, 7 (45), pp.28291 - 28297. ⟨10.1039/c7ra04218c⟩. ⟨hal-01560414⟩

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