Microwave-assisted synthesis and in-vitro anti-tumor activity of 1,3,4-triaryl-5- N-arylpyrazole-carboxamides

Regioselective 1,3-dipolar cycloaddition of nitrilimines with 5-arylidene-2-arylimino-4-thiazolidinones and with 2-(4-arylidene)thiazolo[3,2- a]benzimidazol-3(2 H)-ones afforded the corresponding 1,3,4-triaryl-5- N-arylpyrazole-carboxamides and pyrazolylbenzimidazoles. All reactions were carried out...

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Veröffentlicht in:European journal of medicinal chemistry 2010-06, Vol.45 (6), p.2427-2432
Hauptverfasser: Abdel-Aziz, Hatem A., El-Zahabi, Heba S.A., Dawood, Kamal M.
Format: Artikel
Sprache:eng
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Zusammenfassung:Regioselective 1,3-dipolar cycloaddition of nitrilimines with 5-arylidene-2-arylimino-4-thiazolidinones and with 2-(4-arylidene)thiazolo[3,2- a]benzimidazol-3(2 H)-ones afforded the corresponding 1,3,4-triaryl-5- N-arylpyrazole-carboxamides and pyrazolylbenzimidazoles. All reactions were carried out under conventional thermal heating and/or microwave irradiation. Both the pyrazole-5-carboxamides and pyrazolylbenzimidazoles were examined for their in-vitro anti-tumor activities against two tumor cell lines, Hep-2 and colon CaCo-2. Most of the obtained compounds exhibited significant activity against CaCo-2 and Hep-2 cell lines. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2010.02.026