Hybrid molecules containing a 7-chloro-4-aminoquinoline nucleus and a substituted 2-Pyrazoline with antiproliferative and antifungal activity

Twenty-four new hybrid analogues (15–38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 sho...

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Detalles Bibliográficos
Autores principales: Montoya, Alba, Quiroga, Jairo, Abonia, Rodrigo, Derita, Marcos, Sortino, Maximiliano, Ornelas, Alfredo, Zacchino, Susana, Insuasty, Braulio
Formato: article artículo publishedVersion
Lenguaje:Inglés
Publicado: MDPI 2020
Materias:
Cyclocondensation Reaction
Chalcones
N-aryl-2-pyrazolines
Antifungal Activity
Antiproliferative Activity
Acceso en línea:http://hdl.handle.net/2133/19513
http://hdl.handle.net/2133/19513
Aporte de:
Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) de Universidad Nacional de Rosario
Descripción
Sumario:Twenty-four new hybrid analogues (15–38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 showed significant cytostatic activity, with the most outstanding GI50 values ranging from 0.05 to 0.95 µM. The hybrid compounds (15–38) were also evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. From the obtained results some structure–activity relationships were outlined.

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