Synthesis and biological properties of new 5-nitroindazole derivatives |
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Authors: | Arán 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 |
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Institution: | Instituto de Química Médica, Juan de la Cierva 3, 28006 Madrid, Spain. vjaran@iqm.csic.es |
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Abstract: | A series of new 3-alkoxy- or 3-hydroxy-1-omega-(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 microg/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 microg/mL), loosing cytotoxicity at lower doses. QSAR studies have been carried out. X-ray crystallographic study of compound 8 has been performed. |
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