| Added by | mollevi |
|---|---|
| Last modified by | alainmange |
| Group name | PlateformePP2I |
| Item Type | Journal Article |
| Title | New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships |
| Creator | Zghaib et al. |
| Author | Zahraa Zghaib |
| Author | Jean-François Guichou |
| Author | Johanna Vappiani |
| Author | Nicole Bec |
| Author | Kamel Hadj-Kaddour |
| Author | Laure-Anaïs Vincent |
| Author | Stéphanie Paniagua-Gayraud |
| Author | Christian Larroque |
| Author | Georges Moarbess |
| Author | Pierre Cuq |
| Author | Issam Kassab |
| Author | Mona Diab-Assaf |
| Author | Pierre-Antoine Bonnet |
| Abstract | Microtubules are considered as important targets of anticancer therapy. EAPB0503 and its structural imidazo[1,2-a]quinoxaline derivatives are major microtubule-interfering agents with potent anticancer activity. In this study, the synthesis of several new derivatives of EAPB0503 is described, and the anticancer efficacy of 13 novel derivatives on A375 human melanoma cell line is reported. All new compounds show significant antiproliferative activity with IC50 in the range of 0.077-122?M against human melanoma cell line (A375). Direct inhibition of tubulin polymerization assay in vitro is also assessed. Results show that compounds 6b, 6e, 6g, and EAPB0503 highly inhibit tubulin polymerization with percentages of inhibition of 99%, 98%, 90%, and 84% respectively. Structure-activity relationship studies within the series are also discussed in line with molecular docking studies into the colchicine-binding site of tubulin. |
| Publication | Bioorganic & Medicinal Chemistry |
| Volume | 24 |
| Issue | 11 |
| Pages | 2433-2440 |
| Date | 06 01, 2016 |
| Journal Abbr | Bioorg. Med. Chem. |
| Language | eng |
| DOI | 10.1016/j.bmc.2016.04.004 |
| ISSN | 1464-3391 |
| Short Title | New imidazoquinoxaline derivatives |
| Library Catalog | PubMed |
| Extra | PMID: 27094151 |
| Tags | Antineoplastic Agents, Antiproliferative activity, author, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Human melanoma cancer cell line (A375), Humans, Imidazoles, Imidazo[1,2-a]quinoxaline, Melanoma, Molecular docking, Molecular Docking Simulation, Molecular Structure, original, Polymerization, pp2i, Quinoxalines, Structure - activity relationship, Structure-Activity Relationship, Tubulin, Tubulin depolymerization, Tumor Cells, Cultured |
| Date Added | 2019/06/04 - 17:28:09 |
| Date Modified | 2020/01/14 - 10:25:54 |
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