Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells

Title:Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells

Volume: 10 Issue: 4

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

Affiliation:

Keywords: Norcantharidin, synthesis, antiproliferative activity.

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.

Cite this article as:

Gang Tu Guo, Feng Zhan Jian, Li Lv Qiao, Qi Wang Jia, Hai Kuang Bin and Hua Li Shao, Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells, Medicinal Chemistry 2014; 10 (4) . https://dx.doi.org/10.2174/15734064113099990037