Design, synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole

Xiao-Dong Yang; Wei-Chao Wan; Xiao-Yan Deng; Yan Li; Li-Juan Yang; Liang Li; Hong-Bin Zhang

doi:10.1016/j.bmcl.2012.02.094

Design, synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2726-9. doi: 10.1016/j.bmcl.2012.02.094. Epub 2012 Mar 5.

Authors

Xiao-Dong Yang¹, Wei-Chao Wan, Xiao-Yan Deng, Yan Li, Li-Juan Yang, Liang Li, Hong-Bin Zhang

Affiliation

¹ Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, PR China. [email protected]

PMID: 22440627
DOI: 10.1016/j.bmcl.2012.02.094

Abstract

A series of novel hybrid compounds between 2-phenylbenzofuran and imidazole have been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that substitution of the imidazolyl-3-position with a naphthylacyl or bromophenacyl group, were vital for modulating cytotoxic activity. In particular, hybrid compound 15 was found to be the most potent compound against 4 strains human tumor cell lines and more active than cisplatin (DDP), and exhibited cytotoxic activity selectively against liver carcinoma (SMMC-7721).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Benzofurans / chemical synthesis*
Benzofurans / chemistry
Benzofurans / pharmacology*
Cell Line, Tumor
Cell Survival / drug effects
Cisplatin / therapeutic use
Drug Design*
Humans
Imidazoles / chemical synthesis*
Imidazoles / chemistry
Imidazoles / pharmacology*
Liver Neoplasms / drug therapy
Molecular Structure
Structure-Activity Relationship

Substances

Antineoplastic Agents
Benzofurans
Imidazoles
Cisplatin