title: Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity.
abstract: 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.
authors.affiliation: Grupo de Investigaci&#243;n de Compuestos Heteroc&#237;clicos, Departamento de Qu&#237;mica, Universidad del Valle, A. A. 25360 Cali, Colombia. montoyaarias340@gmail.com.
authors.forename: Alba
authors.initials: A
authors.lastname: Montoya
authors.affiliation: Grupo de Investigaci&#243;n de Compuestos Heteroc&#237;clicos, Departamento de Qu&#237;mica, Universidad del Valle, A. A. 25360 Cali, Colombia. jaiquir@gmail.com.
authors.forename: Jairo
authors.initials: J
authors.lastname: Quiroga
authors.affiliation: Grupo de Investigaci&#243;n de Compuestos Heteroc&#237;clicos, Departamento de Qu&#237;mica, Universidad del Valle, A. A. 25360 Cali, Colombia. rodrigo.abonia@correounivalle.edu.co.
authors.forename: Rodrigo
authors.initials: R
authors.lastname: Abonia
authors.affiliation: &#193;rea Farmacognosia, Facultad de Ciencias Bioqu&#237;micas y Farmac&#233;uticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, Argentina. mgderita@hotmail.com.
authors.forename: Marcos
authors.initials: M
authors.lastname: Derita
authors.affiliation: &#193;rea Farmacognosia, Facultad de Ciencias Bioqu&#237;micas y Farmac&#233;uticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, Argentina. msortino@fbioyf.unr.edu.ar.
authors.forename: Maximiliano
authors.initials: M
authors.lastname: Sortino
authors.affiliation: Department of Chemistry, University of Texas at El Paso, 799689, 500 W. University Ave. El Paso, TX 79902, USA. aornelas3@miners.utep.edu.
authors.forename: Alfredo
authors.initials: A
authors.lastname: Ornelas
authors.affiliation: &#193;rea Farmacognosia, Facultad de Ciencias Bioqu&#237;micas y Farmac&#233;uticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, Argentina. szaabgil@citynet.net.ar.
authors.forename: Susana
authors.initials: S
authors.lastname: Zacchino
authors.affiliation: Grupo de Investigaci&#243;n de Compuestos Heteroc&#237;clicos, Departamento de Qu&#237;mica, Universidad del Valle, A. A. 25360 Cali, Colombia. braulio.insuasty@correounivalle.edu.co.
authors.forename: Braulio
authors.initials: B
authors.lastname: Insuasty
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003455:Cryptococcus neoformans / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000634:Aminoquinolines; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D011720:Pyrazoles; C047186:7-chloro-4-aminoquinoline
keywords: N-aryl-2-pyrazolines; antifungal; antiproliferative activity; chalcones; cyclocondensation reaction