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.