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

Authors: Deng, Liping; yang, Bo; He, Qiaojun; Hu, Yongzhou

Source: Letters in Drug Design & Discovery, Volume 5, Number 3, April 2008 , pp. 225-231(7)

Publisher: Bentham Science Publishers

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Abstract:

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

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018008784083992

Publication date: 2008-04-01

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