Cytotoxic activity of 3-(5-phenyl-3 H -[1,2,4]dithiazol-3-yl)chromen-4-ones and 4-oxo-4 H -chromene-3-carbothioic acid N -phenylamides
| Autor: | Ajit Kumar Saxena, Mohan Paul S. Ishar, Ashish Kapur, Tilak Raj, Richa Kaur Bhatia, Madhunika Sharma |
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| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
Antineoplastic Agents Chemical synthesis Medicinal chemistry Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Drug Discovery Humans Structure–activity relationship Cytotoxicity Thioamide Pharmacology chemistry.chemical_classification Bicyclic molecule biology Organic Chemistry Xylene General Medicine Amides Toluene Thiazoles chemistry Chromones Enzyme inhibitor biology.protein |
| Zdroj: | European Journal of Medicinal Chemistry. 45:790-794 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2009.11.001 |
| Popis: | 6/6,7-Substituted-3-formylchromones (8a-g) were reacted with 2 equivalents thiobenzamide (9) in refluxing toluene to furnish substituted-3-(5-phenyl-3H-[1,2,4]dithiazol-3-yl)chromen-4-ones (10a-g) in high yields. Similarly, when substituted-2-anilino-3-formylchromones (8a-d) were reacted with thiobenzamide (9, 2 equivalents) in refluxing xylene, 4-oxo-4H-chromene-3-carbothioic acid N-phenylamides (11a-d) were obtained in high yields. All the compounds (10a-g) and (11a-d) display significant cytotoxic activity against a number of human cancer cell lines. Among these compounds 10e (IC(50) = 10 microM), 10b (IC(50) = 14.6 microM) and 10a (IC(50) = 10.5 microM) showed maximum cytotoxic activity on neuroblastoma. Also, the compound 10c (IC(50) = 10.5 microM) showed maximum cytotoxic activity on ovarian cancer cell line. |
| Databáze: | OpenAIRE |
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