Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells

Publisher: Bentham Science Publishers

E-ISSN: 1875-6638|10|4|376-381

ISSN: 1573-4064

Source: Medicinal Chemistry, Vol.10, Iss.4, 2014-04, pp. : 376-381

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Abstract

Diels-Alder reaction between furan and maleic anhydride resulted in 5,6-dehydro norcantharidin, then norcantharidinwas obtained by reduction. The substituted-carboxylic acid was condensed with N-aminothiourea in presence ofphosphorus oxychloride, yielding 2-amino-1,3,4-thiadiazole derivatives. Novel norcantharidin derivatives were synthesizedwith 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, lt;supgt;1lt;/supgt;HNMR, ESI-MS and were reported for thefirst 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.