Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells

Author(s): Guo Gang Tu, Jian Feng Zhan, Qiao Li Lv, Jia Qi Wang, Bin Hai Kuang, Shao Hua Li.

Journal Name: Medicinal Chemistry

Volume 10 , Issue 4 , 2014

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Abstract:

Diels-Alder reaction between furan and maleic anhydride resulted in 5,6-dehydro norcantharidin, then norcantharidin was obtained by reduction. The substituted-carboxylic acid was condensed with N-aminothiourea in presence of phosphorus oxychloride, yielding 2-amino-1,3,4-thiadiazole derivatives. Novel norcantharidin derivatives were synthesized with acylation, then intramolecular condensation using norcantharidin (or 5,6-dehydro norcantharidin) and 2-amino- 1,3,4-thiadiazole derivatives. All the target compounds were confirmed by IR, 1HNMR, ESI-MS and were reported for the first time. Norcantharidin derivatives antiproliferative assay was tested by MTT method against A549 and PC-3 cell lines. The results showed that all the norcantharidin derivatives displayed moderate inhibitory activities.

Keywords: Norcantharidin, synthesis, antiproliferative activity.

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Article Details

VOLUME: 10
ISSUE: 4
Year: 2014
Page: [376 - 381]
Pages: 6
DOI: 10.2174/15734064113099990037
Price: $58

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