An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties
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| DC Field | Value | Language |
|---|---|---|
| dc.contributor.author | F Porta | - |
| dc.contributor.author | G Facchetti | - |
| dc.contributor.author | N Ferri | - |
| dc.contributor.author | A Gelain | - |
| dc.contributor.author | F Meneghetti | - |
| dc.contributor.author | S Villa | - |
| dc.contributor.author | D Barlocco | - |
| dc.contributor.author | D Masciocchi | - |
| dc.contributor.author | A Asai | - |
| dc.contributor.author | N Miyoshi | - |
| dc.contributor.author | S Marchiano | - |
| dc.contributor.author | Byoung-Mog Kwon | - |
| dc.contributor.author | Yena Jin | - |
| dc.contributor.author | V Gandin | - |
| dc.contributor.author | C Marzano | - |
| dc.contributor.author | I Rimoldi | - |
| dc.date.accessioned | 2017-08-29 | - |
| dc.date.available | 2017-08-29 | - |
| dc.date.issued | 2017 | - |
| dc.identifier.issn | 0223-5234 | - |
| dc.identifier.uri | 10.1016/j.ejmech.2017.03.017 | ko |
| dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/17073 | - |
| dc.description.abstract | New Pt(II) complexes (Pt-1-3) bearing 1,2,5-oxadiazole ligands (1-3) were synthesized, characterized and evaluated for their ability to disrupt STAT3 dimerization. Ligand 3·HCl showed cytotoxic effects on HCT-116 cells (IC50 = 95.2 μM) and a selective ability to interact with STAT3 (IC50 = 8.2 μM) versus STAT1 (IC50 > 30 μM). Its corresponding platinum complex Pt-3 exhibited an increased cytotoxicity (IC50 = 18.4 μM) and a stronger interaction with STAT3 (IC50 = 1.4 μM), leading to inhibition of its signaling pathway. Pt-3 was also evaluated in cell-based assays for its action on p53 expression and on STAT3 phosphorylation. In syngeneic murine Lewis lung carcinoma (LLC) implanted in C57BL/6 mice, Pt-3 showed a higher antitumor activity with fewer side effects than cisplatin | - |
| dc.publisher | Elsevier | - |
| dc.title | An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties | - |
| dc.title.alternative | An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties | - |
| dc.type | Article | - |
| dc.citation.title | European Journal of Medicinal Chemistry | - |
| dc.citation.number | 0 | - |
| dc.citation.endPage | 206 | - |
| dc.citation.startPage | 196 | - |
| dc.citation.volume | 131 | - |
| dc.contributor.affiliatedAuthor | Byoung-Mog Kwon | - |
| dc.contributor.affiliatedAuthor | Yena Jin | - |
| dc.contributor.alternativeName | Porta | - |
| dc.contributor.alternativeName | Facchetti | - |
| dc.contributor.alternativeName | Ferri | - |
| dc.contributor.alternativeName | Gelain | - |
| dc.contributor.alternativeName | Meneghetti | - |
| dc.contributor.alternativeName | Villa | - |
| dc.contributor.alternativeName | Barlocco | - |
| dc.contributor.alternativeName | Masciocchi | - |
| dc.contributor.alternativeName | Asai | - |
| dc.contributor.alternativeName | Miyoshi | - |
| dc.contributor.alternativeName | Marchiano | - |
| dc.contributor.alternativeName | 권병목 | - |
| dc.contributor.alternativeName | 진예나 | - |
| dc.contributor.alternativeName | Gandin | - |
| dc.contributor.alternativeName | Marzano | - |
| dc.contributor.alternativeName | Rimoldi | - |
| dc.identifier.bibliographicCitation | European Journal of Medicinal Chemistry, vol. 131, pp. 196-206 | - |
| dc.identifier.doi | 10.1016/j.ejmech.2017.03.017 | - |
| dc.subject.keyword | Antitumor agents | - |
| dc.subject.keyword | Cytotoxic activity | - |
| dc.subject.keyword | DNA-interaction | - |
| dc.subject.keyword | Platinum diamine complex | - |
| dc.subject.keyword | Proteinprotein interactions | - |
| dc.subject.local | Anti-tumor agent | - |
| dc.subject.local | Antitumor agents | - |
| dc.subject.local | antitumor agent | - |
| dc.subject.local | cytotoxic activities | - |
| dc.subject.local | cytotoxic activity | - |
| dc.subject.local | Cytotoxic activity | - |
| dc.subject.local | DNA-interaction | - |
| dc.subject.local | Platinum diamine complex | - |
| dc.subject.local | Protein-protein interaction | - |
| dc.subject.local | Proteinprotein interactions | - |
| dc.subject.local | Protein-Protein Interaction | - |
| dc.subject.local | Protein-Protein interaction | - |
| dc.subject.local | protein-protein interaction | - |
| dc.subject.local | Protein-protein interactions | - |
| dc.description.journalClass | Y | - |
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