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Molecules 2016, 21(8), 969; doi:10.3390/molecules21080969

Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity

1
Grupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A. A. 25360 Cali, Colombia
2
Área Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, Argentina
3
Department of Chemistry, University of Texas at El Paso, 799689, 500 W. University Ave. El Paso, TX 79902, USA
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 19 May 2016 / Revised: 18 July 2016 / Accepted: 18 July 2016 / Published: 27 July 2016
View Full-Text   |   Download PDF [5079 KB, uploaded 27 July 2016]   |  

Abstract

Twenty-four new hybrid analogues (1538) 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 (1538) were also evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. From the obtained results some structure–activity relationships were outlined. View Full-Text
Keywords: cyclocondensation reaction; chalcones; N-aryl-2-pyrazolines; antifungal; antiproliferative activity cyclocondensation reaction; chalcones; N-aryl-2-pyrazolines; antifungal; antiproliferative activity
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MDPI and ACS Style

Montoya, A.; Quiroga, J.; Abonia, R.; Derita, M.; Sortino, M.; Ornelas, A.; Zacchino, S.; Insuasty, B. Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity. Molecules 2016, 21, 969.

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