Guo Gang Tu, Jian Feng Zhan, Qiao Li Lv, Jia Qi Wang, Bin Hai Kuang and Shao Hua Li Pages 376 - 381 ( 6 )
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.
Norcantharidin, synthesis, antiproliferative activity.
Department of Medicinal Chemistry, School of Pharmaceutical Science, Nanchang University, 461, BaYi Road, NanChang, 330006, P.R. China.