An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties
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- Title
- An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties
- Author(s)
- F Porta; G Facchetti; N Ferri; A Gelain; F Meneghetti; S Villa; D Barlocco; D Masciocchi; A Asai; N Miyoshi; S Marchiano; Byoung-Mog Kwon; Yena Jin; V Gandin; C Marzano; I Rimoldi
- Bibliographic Citation
- European Journal of Medicinal Chemistry, vol. 131, pp. 196-206
- Publication Year
- 2017
- 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
- Keyword
- Antitumor agentsCytotoxic activityDNA-interactionPlatinum diamine complexProteinprotein interactions
- ISSN
- 0223-5234
- Publisher
- Elsevier
- DOI
- http://dx.doi.org/10.1016/j.ejmech.2017.03.017
- Type
- Article
- Appears in Collections:
- 1. Journal Articles > Journal Articles
- Files in This Item:
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