Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones

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 leuk...

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Detalles Bibliográficos
Autores principales: Onnis, Valentina, Demurtas, Monica, Deplano, Alessandro, Balboni, Gianfranco, Baldisserotto, Anna, Manfredini, Stefano, Pacifico, Salvatore, Liekens, Sandra, Balzarini, Jan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273944/
https://www.ncbi.nlm.nih.gov/pubmed/27144551
http://dx.doi.org/10.3390/molecules21050579
Descripción
Sumario: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 IC(50) values in the low micromolar range.

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