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

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• 作者：Carine Deleuze-Masquefa ; Georges Moarbess ; Sonia Khier ; Nadè ; ge David ; Sté ; phanie Gayraud-Paniagua ; Franç ; oise Bressolle ; Fré ; dé ; ric Pinguet ; Pierre-Antoine Bonnet
• 关键词：Imidazoquinoxalines ; Imiquimod ; Melanoma ; In vitro activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：September 2009
• 年：2009
• 卷：44
• 期：9
• 页码：3406-3411
• 全文大小：186 K

文摘

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.