Design, synthesis and evaluation of antiproliferative activity of new benzimidazolehydrazones

ONNIS, VALENTINA;DEMURTAS, MONICA;DEPLANO, ALESSANDRO;BALBONI, GIANFRANCO;Baldisserotto, A;Manfredini, S;Pacifico, S;Liekens, S;Balzarini, J.

2016-01-01

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Abstract

The synthesis and antiproliferative activity of new benzimidazole derivatives bearing an hydrazone mojety at the 2-position is described. The new N1-(4-arylidene)-1H-benzo[d]imidazole-2- carbohydrazides were evaluated for their cytostatic activity toward the murine leukemia (L1210), human T-cell leukemia (CEM), human cervix carcinoma (HeLa) and human pancreas carcinoma cells (Mia Paca-2). A preliminary structure-activity relationship could be defined. Some of the compounds possess encouraging and consistent antiproliferative activity, having IC50 values in the low micromolar range