Letters in Drug Design & Discovery

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


Disodium Phosphate of Norcantharidin Analogues: Design, Synthesis and their Anticancer Evaluation

Author(s): Liping Deng, Yongmiao Shen, Wei Wang, Weifeng Tao, Jianguo Lv, Chunlei Wu.


To design and synthesize disodium phosphate of novel norcanthridin analogues. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumour cell lines: SMMC-7721, SGC7901, ECA109, A549 and MCF-7 producing IC50 values from 0.15 μM to > 50 μM. Compounds 6 and 17 showed potency for the treatment of mammary adenocarcinoma, with IC value to MCF-7 cell line comparable to that of cantharidin, which proves that the phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.

Keywords: Norcantharidin analogues, Phosphorylation, Anticancer evaluation, Solubility

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Article Details

Year: 2009
Page: [345 - 352]
Pages: 8
DOI: 10.2174/1570180810906050345
Price: $58