Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones

作者:Onnis Valentina; Demurtas Monica; Deplano Alessandro; Balboni Gianfranco; Baldisserotto Anna; Manfredini Stefano; Pacifico Salvatore; Liekens Sandra; Balzarini Jan
来源:Molecules, 2016, 21(5): 579.
DOI:10.3390/molecules21050579

摘要

The synthesis and antiproliferative activity of new benzimidazole derivatives bearing an hydrazone mojety at the 2-position is described. The new N'-(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.