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Synthesis and biological properties of new 5-nitroindazole derivatives

AuthorsArán, Vicente J. ; Ochoa, Carmen; Boiani, Lucía; Buccino, Pablo; Cerecetto, Hugo; Gerpe, Alejandra; González, Mercedes; Montero, David; Nogal, Juan José; Gómez-Barrio, Alicia; Azqueta, Amaya; López De Ceráin, Adela; Piro, Oscar E.; Castellano, Eduardo E.
Issue Date2005
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry 13: 3197- 3207 (2005)
AbstractA 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. © 2005 Elsevier Ltd. All rights reserved.
Identifiersdoi: 10.1016/j.bmc.2005.02.043
issn: 0968-0896
e-issn: 1464-3391
Appears in Collections:(IQM) Artículos
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