Author/Authors :
Vicente J. Ar?n، نويسنده , , Carmen Ochoa، نويسنده , , Luc??a Boiani، نويسنده , , Pablo Buccino، نويسنده , , Hugo Cerecetto، نويسنده , , Alejandra Gerpe، نويسنده , , Mercedes Gonzalez-Wangüemert، نويسنده , , David Montero Pereira، نويسنده , , Juan José Nogal-Ruiz، نويسنده , , Alicia G?mez-Barrio، نويسنده , , Amaya Azqueta، نويسنده , , Adela L?pez de Cer?in، نويسنده , , Oscar E. Piro، نويسنده , , Eduardo E. Castellano، نويسنده ,
Abstract :
A series of new 3-alkoxy- or 3-hydroxy-1-[ω-(dialkylamino)alkyl]-5-nitroindazoles have been synthesized and their trichomonacidal, antichagasic and antineoplastic properties studied. Five derivatives (5, 6, 8, 9 and 17) showed remarkable trichomonacidal activity against Trichomonas vaginalis at 10 μg/mL concentration. Three compounds (8, 10, 11) exhibited interesting antichagasic activity and these same compounds moderate antineoplastic activity against TK-10 and HT-29 cell lines. Unspecific cytotoxicity against macrophages has also been evaluated and only compounds 9, 10 and 11 resulted cytotoxic at the higher dose evaluated (100 μg/mL), loosing cytotoxicity at lower doses. QSAR studies have been carried out. X-ray crystallographic study of compound 8 has been performed.
Keywords :
QSAR , 5-Nitroindazoles , Synthesis , Antiprotozoal and antineoplastic activities
