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Xie W.,Hunan University of Science and Technology | Xie W.,Hunan University | Xie S.,Hunan University of Humanities, Science and Technology | Zhou Y.,Hunan University of Science and Technology | And 8 more authors.
European Journal of Medicinal Chemistry

A series of 5,6-disubstituted pyridine-2,3-dione-3-thiosemicarbazone derivatives(2a-2n) and 5,6-disubstituted pyridine-2,3-dione S-benzyl-3- thiosemicarbazones(3a-3g) were synthesized starting from 2,3-dihydroxypyridine via oxidation-Michael additions, condensations and nucleophilic substitutions. The structures of the compounds were established by IR, 1H NMR, 13C NMR, and HRMS. All newly synthesized compounds were screened for their anticancer activity against Breast cancer (MCF-7), Colon cancer (HCT-116) and hepatocellular cancer (BEL7402) cell lines. Bioassay results indicated that most of the prepared compounds exhibited cytotoxicity against various cancer cells in vitro. Some of the compounds exhibited promising antiproliferative activity, which were comparable to the positive control (5-fluorouracil). The structure-activity relationship was discussed. © 2014 Elsevier Masson SAS. All rights reserved. Source

Xie W.,Hunan University of Science and Technology | Xie W.,Sun Yat Sen University | Xie W.,Shenzhen Hanyu Pharmaceutical Co. | Liu J.,Shenzhen Hanyu Pharmaceutical Co. | And 3 more authors.
Journal of Peptide Science

Four novel octreotide analogs with cell-penetrating peptides (CPPs) at the N-terminus or C-terminus were synthesized by a stepwise Fmoc solid-phase synthesis strategy. The synthesized peptides were analyzed and characterized using reverse phase HPLC and MALDI-TOF mass spectrometry. The antiproliferative activity of the analogswas tested in vitro onhumangastric (SGC-7901) and hepatocellular cancer (BEL7402) cell lines using the 3-(4,5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Interestingly, these analogs showed a higher anticancer activities than the parent octreotide except CMTPT03 analog. The results demonstrate that the designed octreotide analogs enhance their anticancer activity after linking together the CPPs to octreotide at the N-terminus, and are potential molecules for future use in cancer therapy and drug targeting. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd. Source

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