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

Carine Deleuze-Masquéfa (1) , Georges Moarbess (2) , Sonia Khier , Nadège David (3) , Stéphanie Gayraud-Paniagua (3) , Françoise Bressolle , Frédéric Pinguet (4) , Pierre-Antoine Bonnet (1)

1 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]
2 LU / ULB - الجامعة اللبنانية [بيروت] = Lebanese University [Beirut] = Université libanaise [Beyrouth]
3 LCBE - Laboratoire de Chimie des Biomolécules et de l'Environnement
4 CRLCC Val d'Aurelle - Paul Lamarque

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.

Keywords: Antitumor; Drugs screening; Melanoma

Domains: Pharmacology; Medication; Pharmaceutical sciences

Carine Deleuze-Masquéfa, Georges Moarbess, Sonia Khier, Nadège David, Stéphanie Gayraud-Paniagua, et al.. New imidazo[1,2-a]quinoxaline derivatives: Synthesis and in vitro activity against human melanoma. European Journal of Medicinal Chemistry, 2009, 44 (9), pp.3406-3411. ⟨10.1016/j.ejmech.2009.02.007⟩. ⟨hal-02309640⟩