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.
Letters in Drug Design & Discovery
Title:Novel Tricyclic Indeno[5,6-b]furan-imidazole Hybrid Compounds: Design, Synthesis and Antitumor Activity
Volume: 10 Issue: 7
Author(s): Wen Chen, Li-Juan Yang, Yan Li, Xue-Quan Wang, Shao-Jie Wang, Wei-Chao Wan, Hong- Bin Zhang and Xiao-Dong Yang
Affiliation:
Keywords: Hybrid compound, Imidazole, Indeno[5, 6-b]furan, Synthesis, Cytotoxic activity, Structure–activity relationships.
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.
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Cite this article as:
Chen Wen, Yang Li-Juan, Li Yan, Wang Xue-Quan, Wang Shao-Jie, Wan Wei-Chao, Zhang Hong- Bin and Yang Xiao-Dong, Novel Tricyclic Indeno[5,6-b]furan-imidazole Hybrid Compounds: Design, Synthesis and Antitumor Activity, Letters in Drug Design & Discovery 2013; 10 (7) . https://dx.doi.org/10.2174/1570180811310070003
DOI https://dx.doi.org/10.2174/1570180811310070003 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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