Novel tricyclic indeno[5,6-b]furan-imidazole hybrid compounds: Design, synthesis and antitumor activity

LETTERS IN DRUG DESIGN & DISCOVERY(2013)

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摘要
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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关键词
Hybrid compound,Imidazole,Indeno[5,6-b]furan,Synthesis,Cytotoxic activity,Structure-activity relationships
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