New imidazo[1,2- a]quinoxaline derivatives: Synthesis and in vitro activity against human melanoma

New imidazo[1,2- a]quinoxaline analogues have been synthesized in good yields via a bimolecular condensation of 2-imidazole carboxylic acid, followed by a coupling with ortho-fluoroaniline and subsequent substitution on the imidazole ring by Suzuki Cross-coupling reaction using microwave assistance....

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Bibliographic Details
Published in:European journal of medicinal chemistry 2009-09, Vol.44 (9), p.3406-3411
Main Authors: Deleuze-Masquefa, Carine, Moarbess, Georges, Khier, Sonia, David, Nadège, Gayraud-Paniagua, Stéphanie, Bressolle, Françoise, Pinguet, Frédéric, Bonnet, Pierre-Antoine
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
Cell Proliferation - drug effects
Drug Screening Assays, Antitumor
General aspects
Humans
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Imidazoquinoxalines
Imiquimod
In vitro activity
Life Sciences
Medical sciences
Medication
Melanoma
Melanoma - drug therapy
Pharmaceutical sciences
Pharmacology
Pharmacology. Drug treatments
Quinoxalines - chemical synthesis
Quinoxalines - chemistry
Quinoxalines - pharmacology
Structure-Activity Relationship
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Summary:New imidazo[1,2- a]quinoxaline analogues have been synthesized in good yields via a bimolecular condensation of 2-imidazole carboxylic acid, followed by a coupling with ortho-fluoroaniline and subsequent substitution on the imidazole ring by Suzuki Cross-coupling reaction using microwave assistance. Antitumor activities of these derivatives were evaluated by growth inhibition of A375 cells in vitro. All compounds exhibited high activities compared to imiquimod and fotemustine used as references. [Display omitted] IC 50 against A375: 0.20 ± 0.09 μM.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2009.02.007