Cytotoxic activity of 3-(5-phenyl-3H-[1,2,4]dithiazol-3-yl)chromen-4-ones and 4-oxo-4H-chromene-3-carbothioic acid N-phenylamides
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 thiobe...
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Veröffentlicht in: | European journal of medicinal chemistry 2010-02, Vol.45 (2), p.790-794 |
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Sprache: | eng |
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Zusammenfassung: | 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. |
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ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2009.11.001 |