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. 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.
Deleuze-Masquefa
Carine
C
EA 4215, Laboratoire de Chimie des Biomolécules et de l'Environnement, Pharmacochimie et Biomolécules, Université Montpellier I, Faculté de Pharmacie, 15 av. Charles Flahault, BP 14491, 34 093 Montpellier Cedex 5, France. carine.masquefa@univ-montp1.fr
Moarbess
Georges
G
Khier
Sonia
S
David
Nadège
N
Gayraud-Paniagua
Stéphanie
S
Bressolle
Françoise
F
Pinguet
Frédéric
F
Bonnet
Pierre-Antoine
PA
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008545:Melanoma / Q000188:drug therapy*; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007093:Imidazoles; D011810:Quinoxalines; C029899:imidazole