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Synthesis and Anti‐proliferative Activity of Novel Polysubstitued Indazole Derivatives
Authors:Oulemda Bassou  Hakima Chicha  Afaf Allam  Massimiliano Monticone  Rosaria Gangemi  Irena Maric  Maurizio Viale  El Mostapha Rakib
Abstract:A simple and efficient process is developed for the synthesis of new N‐(1‐alkyl‐3‐chloro‐4‐ethoxy‐1H‐indazol‐5‐yl)‐arylsulfonamides 4a – d and N‐(1‐alkyl‐3‐chloro‐1H‐indazol‐5‐yl)‐arylsulfonamides 5a – d through the reduction of 1‐alkyl‐3‐chloro‐5‐nitroindazoles 2a , b with SnCl2 in ethanol followed by coupling the corresponding amine with arylsulfonyl chlorides in pyridine. All the newly synthesized compounds have been characterized by elemental analysis and spectroscopic data. Some compounds were tested for their in vitro antiproliferative activities against two selected human cancer cell lines A2780 and A549. Among all of these derivatives, compound 5d showed the most potent antiproliferative activity against A2780 (IC50 = 5.47 ± 1.45 μM) and A549 (IC50 = 7.73 ± 1.66 μM) cell lines.
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