作者
Vicente J Arán, Carmen Ochoa, Lucıa Boiani, Pablo Buccino, Hugo Cerecetto, Alejandra Gerpe, Mercedes González, David Montero, Juan José Nogal, Alicia Gómez-Barrio, Amaya Azqueta, Adela Lopez de Ceráin, Oscar E Piro, Eduardo E Castellano
发表日期
2005/5/2
期刊
Bioorganic & medicinal chemistry
卷号
13
期号
9
页码范围
3197-3207
出版商
Pergamon
简介
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 10μg/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 (100μg/mL), loosing cytotoxicity at lower doses. QSAR studies have been carried out. X-ray crystallographic study of compound 8 has been performed.
引用总数
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VJ Arán, C Ochoa, L Boiani, P Buccino, H Cerecetto… - Bioorganic & medicinal chemistry, 2005