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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Research Article

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 and Shao Hua Li

Volume 10, Issue 4, 2014

Page: [376 - 381] Pages: 6

DOI: 10.2174/15734064113099990037

Price: $65

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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