Synthesis, antitumor activity and SAR study of novel [1,2,4]triazino[4,5-a]benzimidazole derivatives

Hala Bakr El-Nassan

doi:10.1016/j.ejmech.2012.03.028

Synthesis, antitumor activity and SAR study of novel [1,2,4]triazino[4,5-a]benzimidazole derivatives

Eur J Med Chem. 2012 Jul:53:22-7. doi: 10.1016/j.ejmech.2012.03.028. Epub 2012 Mar 23.

Author

Hala Bakr El-Nassan¹

Affiliation

¹ Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kasr El-Aini Street, Cairo 11562, Egypt. [email protected]

PMID: 22542105
DOI: 10.1016/j.ejmech.2012.03.028

Abstract

A series of novel 1,2,3,4-tetrahydro[1,2,4]triazino[4,5-a]benzimidazoles carrying variety of aryl and heteroaryl groups at position 1 were synthesized. The newly synthesized compounds were tested in vitro on human breast adenocarcinoma cell line (MCF7). Some of the test compounds showed potent antitumor activity, especially compound 3c [1-(2-chlorophenyl) derivative] which displayed the highest activity among the test compounds.

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Benzimidazoles / chemical synthesis*
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Cell Line, Tumor
Chemistry Techniques, Synthetic
Drug Screening Assays, Antitumor
Humans
Structure-Activity Relationship

Substances

Antineoplastic Agents
Benzimidazoles