Synthesis, structural characterization and anticancer evaluation of pyrazole derivatives
The utility of 4-isothiocyanato- N -(1-phenyl-1 H -pyrazol-5-yl)benzene sulfonamide 2 in the synthesis of some novel thiosemicarbazide, carbamothioate,1,3,4-thiadiazole, azomethine, thiourea, bisthiourea and imidazole derivatives is reported. The structure of the newly synthesized compounds was conf...
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Veröffentlicht in: | Medicinal chemistry research 2018, Vol.27 (1), p.72-79 |
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Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | The utility of 4-isothiocyanato-
N
-(1-phenyl-1
H
-pyrazol-5-yl)benzene sulfonamide
2
in the synthesis of some novel thiosemicarbazide, carbamothioate,1,3,4-thiadiazole, azomethine, thiourea, bisthiourea and imidazole derivatives is reported. The structure of the newly synthesized compounds was confirmed on the basis of analytical and spectral data. Some of the prepared compounds were evaluated for their in vitro anticancer activity against Ehrlich ascites carcinoma cells (EAC). It was found that the corresponding 2-acetyl-
N
-(4
-(N
-(1-phenyl-1
H
-pyrazol-5-yl) sulfamoyl)phenyl) hydrazinecarbothioamide
7
with IC
50
value (2.14 µg/ml) showed better activity than doxorubicin with IC
50
value (43.6 µg/ml) as reference drug.
Graphical Abstract
New thiosemicarbazide,carbamothioate,1,3,4-thiadiazole, azomethine, thiourea, bisthiourea and imidazole derivatives containing pyrazole moiety have been synthesized and evaluated for their anticancer activity. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-017-2035-2 |