Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates.

Autor: Kumar N; Department of Chemistry, University of Delhi, Delhi 110007, India., Khan SI, Atheaya H, Mamgain R, Rawat DS
Jazyk: angličtina
Zdroj: European journal of medicinal chemistry [Eur J Med Chem] 2011 Jul; Vol. 46 (7), pp. 2816-27. Date of Electronic Publication: 2011 Apr 15.
DOI: 10.1016/j.ejmech.2011.04.002
Abstrakt: A series of tetraoxanes, tetraoxane-amine and tetraoxane-amide conjugates have been synthesized and screened for in vitro antimalarial activity against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Most of the conjugates showed slightly better antimalarial activity than the parent tetraoxanes. Three of the conjugate compounds were potentially active with IC(50) values in the range of 0.38-0.80μM. Cytotoxicity of four selected compounds was also evaluated in a panel of four cancer (SK-MEL, KB, BT-549, SK-OV-3) and two non-cancer (Vero and LLC-PK(11)) cell lines up to a concentration of 25μM and none of the compounds was found toxic to any of the cells.
(Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
Databáze: MEDLINE
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