title: Synthesis and antiproliferative assay of norcantharidin derivatives in cancer cells.
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, (1)HNMR, 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.
authors.forename: Guo Gang
authors.initials: GG
authors.lastname: Tu
authors.forename: Jian Feng
authors.initials: JF
authors.lastname: Zhan
authors.forename: Qiao Li
authors.initials: QL
authors.lastname: Lv
authors.forename: Jia Qi
authors.initials: JQ
authors.lastname: Wang
authors.forename: Bin Hai
authors.initials: BH
authors.lastname: Kuang
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Science, Nanchang University, 461, BaYi Road, NanChang, 330006, P.R. China. tugg199@yahoo.com.
authors.forename: Shao Hua
authors.initials: SH
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; C069741:norcantharidin