European Journal of Medicinal Chemistry p. 378 - 393 (2014)
Update date:2022-08-04
Topics:
Ronga, Luisa
Del Favero, Marco
Cohen, Anita
Soum, Claire
Le Pape, Patrice
Savrimoutou, Solène
Pinaud, No?l
Mullié, Catherine
Daulouede, Sylvie
Vincendeau, Philippe
Farvacques, Natacha
Agnamey, Patrice
Pagniez, Fabrice
Hutter, Sébastien
Azas, Nadine
Sonnet, Pascal
Guillon, Jean
A series of new 4-alkapolyenylpyrrolo[1,2-a]quinoxaline derivatives, original and structural analogues of alkaloid chimanine B and of previously described 4-alkenylpyrrolo[1,2-a]quinoxalines, was synthesized in good yields using efficient palladium-catalyzed Suzuki-Miyaura cross-coupling reactions. These new compounds were tested for in vitro antiparasitic activity upon three Leishmania spp. strains. Biological results showed activity against the promastigote forms of L. major, L. mexicana and L. donovani with IC50 ranging from 1.2 to 14.7 μM. In attempting to investigate if our pyrrolo[1,2-a]quinoxaline derivatives are broad-spectrum antiprotozoal compounds activities toward one Trypanosoma brucei brucei strain and the W2 and 3D7 Plasmodium falciparum strains were also investigated. In parallel, the in vitro cytotoxicity of these molecules was assessed on the murine J774 and human HepG2 cell lines. Structure-activity relationships of these new synthetic compounds are here discussed.
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