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Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells

[ Vol. 10 , Issue. 4 ]

Author(s):

Guo Gang Tu, Jian Feng Zhan, Qiao Li Lv, Jia Qi Wang, Bin Hai Kuang and Shao Hua Li   Pages 376 - 381 ( 6 )

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.

Affiliation:

Department of Medicinal Chemistry, School of Pharmaceutical Science, Nanchang University, 461, BaYi Road, NanChang, 330006, P.R. China.



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