Abstract
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
Letters in Drug Design & Discovery
Title: Disodium Phosphate of Norcantharidin Analogues: Design, Synthesis and their Anticancer Evaluation
Volume: 6 Issue: 5
Author(s): Liping Deng, Yongmiao Shen, Wei Wang, Weifeng Tao, Jianguo Lv and Chunlei Wu
Affiliation:
Keywords: Norcantharidin analogues, Phosphorylation, Anticancer evaluation, Solubility
Abstract: 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.
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Cite this article as:
Deng Liping, Shen Yongmiao, Wang Wei, Tao Weifeng, Lv Jianguo and Wu Chunlei, Disodium Phosphate of Norcantharidin Analogues: Design, Synthesis and their Anticancer Evaluation, Letters in Drug Design & Discovery 2009; 6 (5) . https://dx.doi.org/10.2174/1570180810906050345
DOI https://dx.doi.org/10.2174/1570180810906050345 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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