Novel 1, 2, 3-Triazole-Linked Norcantharidin Analogues: Synthesis and Evaluation of Growth Inhibition in a Panel of Selected Tumor-Cell Lines

Author(s): Liping Deng, Bo yang, Qiaojun He, Yongzhou Hu

Journal Name: Letters in Drug Design & Discovery

Volume 5 , Issue 3 , 2008

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Twenty-one 1, 2, 3-triazole-linked norcantharidin analogues have been synthesized by the efficient [3+2]1, 3- dipolar cycloaddition reaction of norcantharidin derivatives with three organic azides. All analogues have been screened for their antiproliferative activity against a panel of tumor cell lines: KB, SMMC-7721, SGC7901, ECA109, HO8910 and K562. Compound 8e showed potency for the treatment of hepatoma, with GI50 value (19.0±0.2μM) to SMMC-7721 cell line comparable to that of cantharidin (GI50 value =33.2±0.3μM).

Keywords: 1, 2, 3-Triazole-linked, Cantharidin, Norcantharidin analogues, Cycloaddition, Tumor cell lines, Growth inhibition

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Article Details

Year: 2008
Page: [225 - 231]
Pages: 7
DOI: 10.2174/157018008784083992
Price: $65

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