Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Novel Tricyclic Indeno[5,6-b]furan-imidazole Hybrid Compounds: Design, Synthesis and Antitumor Activity

Author(s): Wen Chen, Li-Juan Yang, Yan Li, Xue-Quan Wang, Shao-Jie Wang, Wei-Chao Wan, Hong- Bin Zhang, Xiao-Dong Yang.

Abstract:

A series of novel hybrid compounds between tricyclic indeno[5,6-b]furan and imidazole has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl group were vital for modulating cytotoxic activity. In particular, hybrid compound 26 was found to be the most potent compound against 5 strains human tumor cell lines and more active than cisplatin (DDP), while compound 18 was more selective towards breast carcinoma (MCF-7) and colon carcinoma (SW480) with IC50 value 3.4-fold and 4.3-fold more sensitive to DDP.

Keywords: Hybrid compound, Imidazole, Indeno[5, 6-b]furan, Synthesis, Cytotoxic activity, Structure–activity relationships.

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Article Details

VOLUME: 10
ISSUE: 7
Year: 2013
Page: [561 - 571]
Pages: 11
DOI: 10.2174/1570180811310070003
Price: $58