کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1315826 | 1499428 | 2016 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Topoisomerase I inhibition and DNA cleavage by zinc, copper, and nickel derivatives of 2-[2-bromoethyliminomethyl]-4-[ethoxymethyl]phenol complexes exhibiting anti-proliferation and anti-metastasis activity Topoisomerase I inhibition and DNA cleavage by zinc, copper, and nickel derivatives of 2-[2-bromoethyliminomethyl]-4-[ethoxymethyl]phenol complexes exhibiting anti-proliferation and anti-metastasis activity](/preview/png/1315826.png)
• Schiff base ligand containing ethoxy and bromoethyl group was prepared.
• Zn, Cu, and Ni complexes of above Schiff base were synthesized and characterized.
• These complexes were able to inhibit topoisomerase I activity and cleave/bind DNA.
• These complexes also showed dual actions: anti-proliferation and anti-metastasis.
• Cu complex exhibited relatively greater activity than Zn and Ni analogs.
Three transition metal derivatives (Zn, Cu, and Ni) of 2-[2-bromoethyliminomethyl]-4-[ethoxymethyl]phenol (L) were synthesized by the reaction of the metal salts with the Schiff base ligand in one pot. In the crystal structure of [Zn(L)Br], the Schiff base ligand binds to the metal center through its phenolate oxygen and imine nitrogen, and adopts a distorted tetrahedral geometry. These compounds were found to inhibit topoisomerase I (topo I) activity, induce DNA cleavage and show DNA binding activity. Moreover, these compounds were found to be cytotoxic towards several cancer cell lines (A2780, MCF-7, HT29, HepG2, A549, PC3, LNCaP) and prevent metastasis of PC3. Collectively, Cu(II) complex 2 shows superior activity relative to its Zn(II) and Ni(II) analogs.
These complexes were able to aim multiple targets (inhibit topoisomerase I activity and cleave/bind DNA) and showed dual actions: anti-proliferation and anti-metastasis.Figure optionsDownload as PowerPoint slide
Journal: Journal of Inorganic Biochemistry - Volume 159, June 2016, Pages 14–21