Chemical stability of the peroxide bond enables diversified synthesis of potent tetraoxane antimalarials.
J Med Chem
; 51(7): 2261-6, 2008 Apr 10.
Article
en En
| MEDLINE
| ID: mdl-18330976
ABSTRACT
Of 17 prepared 1,2,4,5-tetraoxacyclohexanes stable to reductive and acidic conditions, 3 of them were more active than artemisinin against CQ and MFQ resistant strain TM91C235 and all compounds were more active in vitro against W2 than against D6 strain. In vivo, amines 10 and 11a cured all mice at higher doses with MCD < or = 37.5 (mg/kg)/day. Triol 13 was exceptionally active against melanoma (LOX IMVI) and ovarian cancer (IGROV1), both with LC 50 = 60 nM.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Peróxidos
/
Plasmodium falciparum
/
Tetraoxanos
/
Antimaláricos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2008
Tipo del documento:
Article