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 showed...
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MDPI AG
2016-07-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/21/8/969 |
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| author | Alba Montoya Jairo Quiroga Rodrigo Abonia Marcos Derita Maximiliano Sortino Alfredo Ornelas Susana Zacchino Braulio Insuasty |
| author_facet | Alba Montoya Jairo Quiroga Rodrigo Abonia Marcos Derita Maximiliano Sortino Alfredo Ornelas Susana Zacchino Braulio Insuasty |
| author_sort | Alba Montoya |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-23T11:29:43Z |
| format | Article |
| id | doaj.art-46d6f0d36f764050a0525dd8e93797be |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-23T11:29:43Z |
| publishDate | 2016-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-46d6f0d36f764050a0525dd8e93797be2022-12-21T17:48:50ZengMDPI AGMolecules1420-30492016-07-0121896910.3390/molecules21080969molecules21080969Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal ActivityAlba Montoya0Jairo Quiroga1Rodrigo Abonia2Marcos Derita3Maximiliano Sortino4Alfredo Ornelas5Susana Zacchino6Braulio Insuasty7Grupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A. A. 25360 Cali, ColombiaGrupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A. A. 25360 Cali, ColombiaGrupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A. A. 25360 Cali, ColombiaÁrea Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, ArgentinaÁrea Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, ArgentinaDepartment of Chemistry, University of Texas at El Paso, 799689, 500 W. University Ave. El Paso, TX 79902, USAÁrea Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000 Rosario, ArgentinaGrupo de Investigación de Compuestos Heterocíclicos, Departamento de Química, Universidad del Valle, A. A. 25360 Cali, ColombiaTwenty-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.http://www.mdpi.com/1420-3049/21/8/969cyclocondensation reactionchalconesN-aryl-2-pyrazolinesantifungalantiproliferative activity |
| spellingShingle | Alba Montoya Jairo Quiroga Rodrigo Abonia Marcos Derita Maximiliano Sortino Alfredo Ornelas Susana Zacchino Braulio Insuasty Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity Molecules cyclocondensation reaction chalcones N-aryl-2-pyrazolines antifungal antiproliferative activity |
| title | Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity |
| title_full | Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity |
| title_fullStr | Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity |
| title_full_unstemmed | Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity |
| title_short | Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity |
| title_sort | hybrid molecules containing a 7 chloro 4 aminoquinoline nucleus and a substituted 2 pyrazoline with antiproliferative and antifungal activity |
| topic | cyclocondensation reaction chalcones N-aryl-2-pyrazolines antifungal antiproliferative activity |
| url | http://www.mdpi.com/1420-3049/21/8/969 |
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