Cargando…

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...

Descripción completa

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:
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
_version_ 1783377503930286080
author Onnis, Valentina
Demurtas, Monica
Deplano, Alessandro
Balboni, Gianfranco
Baldisserotto, Anna
Manfredini, Stefano
Pacifico, Salvatore
Liekens, Sandra
Balzarini, Jan
author_facet Onnis, Valentina
Demurtas, Monica
Deplano, Alessandro
Balboni, Gianfranco
Baldisserotto, Anna
Manfredini, Stefano
Pacifico, Salvatore
Liekens, Sandra
Balzarini, Jan
author_sort Onnis, Valentina
collection PubMed
description 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.
format Online
Article
Text
id pubmed-6273944
institution National Center for Biotechnology Information
language English
publishDate 2016
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62739442018-12-28 Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones Onnis, Valentina Demurtas, Monica Deplano, Alessandro Balboni, Gianfranco Baldisserotto, Anna Manfredini, Stefano Pacifico, Salvatore Liekens, Sandra Balzarini, Jan Molecules Article 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. MDPI 2016-04-30 /pmc/articles/PMC6273944/ /pubmed/27144551 http://dx.doi.org/10.3390/molecules21050579 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Onnis, Valentina
Demurtas, Monica
Deplano, Alessandro
Balboni, Gianfranco
Baldisserotto, Anna
Manfredini, Stefano
Pacifico, Salvatore
Liekens, Sandra
Balzarini, Jan
Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
title Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
title_full Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
title_fullStr Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
title_full_unstemmed Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
title_short Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones
title_sort design, synthesis and evaluation of antiproliferative activity of new benzimidazolehydrazones
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273944/
https://www.ncbi.nlm.nih.gov/pubmed/27144551
http://dx.doi.org/10.3390/molecules21050579
work_keys_str_mv AT onnisvalentina designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT demurtasmonica designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT deplanoalessandro designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT balbonigianfranco designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT baldisserottoanna designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT manfredinistefano designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT pacificosalvatore designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT liekenssandra designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones
AT balzarinijan designsynthesisandevaluationofantiproliferativeactivityofnewbenzimidazolehydrazones