Antitumor platinum(II) complexes of N-cyclobutyl-1R, 2R-diaminocyclohexane with dicarboxylates as leaving groups. Issue 2 (15th January 2015)

• Record Type: Journal Article
• Authors: Xu, Gang; Zhao, Jian; Gou, Shaohua; Pang, Jie
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 2(2015)
• Page Start: 221
• Page End: 224
• Publication Date: 2015-01-15
• Subjects: Anticancer platinum(II) complexes -- N-Cyclobutyl-1R, 2R-diaminocyclohexane -- Cytotoxicity -- DNA cleavage; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2014.11.069
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Four platinum(II) complexes of N -cyclobutyl- 1R, 2R -diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1, 1-cyclobutanedicarboxylate and4 3-hydroxy-1, 1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and 1 HNMR spectra together with ESI-MS spectroscopy. All complexes showed considerable cytotoxicity against the tested four human tumor cell lines including A549, HCT-116, HepG-2 and MCF-7. Especially, complex4 showed good cytotoxicity against A549 (IC50 = 3.5 μM) and HCT-116 (IC50 = 0.9 μM) cancer cell lines. Moreover, complex3 is the most effective agent among the tested compounds against MCF-7 cell line (IC50 = 1.1 μM). The DNA binding behavior of both complexes3 and4, studied by agarose gel electrophoresis, revealed that they bound to DNA in almost the same way as cisplatin.