1240046-48-3Relevant academic research and scientific papers
CYCLOBUTAN-1,1 -DICARBOXYLATO COMPLEXES OF PLATINUM WITH N6-BENZYLADENINE DERIVATIVES, METHOD OF THEIR PREPARATION AND APPLICATION OF THESE COMPLEXES AS DRUGS IN ANTITUMOUR THERAPY
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Page/Page column 13-14, (2011/04/18)
Cyclobutane-1,1-dicarboxylato complexes of platinum in the oxidation state +II and their crystal-solvates including the structural motif I or having the general formula Il expressed by the structural formula [Pt(cbdc)(L)2] Il or the general for
In vitro cytotoxic-active platinum(II) complexes derived from carboplatin and involving purine derivatives
Dvorak, Lukas,Popa, Igor,Starha, Pavel,Travnicek, Zdenek
, p. 3441 - 3448 (2011/01/06)
Six platinum(II) complexes of the general formula [Pt(cbdc)-(HL n)2] (1-6; cbdc = cyclobutane-1,1-dicarboxylate and HL1-HL6 = benzyl-substituted 6-benzylamino-2-chloro-9- isopropylpurine derivatives) have been synthesized by the reaction of [Pt(cbdc)(dmso)2] with the corresponding HLn compound. The prepared complexes were characterized by elemental analysis and FTIR, Raman and NMR (1H, 13C, 15N and 195Pt) spectroscopy. Based on the results of these techniques, it can be concluded that the central PtII atom of the complexes 1-6 is coordinated to two oxygen atoms originating from the cyclobutane-1,1-dicarboxylate group and to two nitrogen atoms from two HLn molecules, that is, having a PtN2O2 donor set. Detailed multinuclear and two-dimensional NMR studies indicated the N-7 atom to be the coordination site of the purine derivatives. The coordination mode was proven by a single-crystal X-ray analysis of the [Pt(cbdc)(dmso)- (HL7)]·H2O (7a.H2O) intermediate [HL7 = 2-chloro-6-(2-methoxybenzyl)amino-9- isopropylpurine]. The geometry is slightly distorted square-planar and the central PtII atom is coordinated to one bidentate cyclobutane-1,1-dicarboxylate dianion, one dmso molecule through the sulfur atom and one HL7 molecule through the N-7 atom of the purine ring, that is, with a PtNO2S donor set. The complexes 1-6 were tested for their in vitro cytotoxicity against K-562 (chronic myelogenous leukaemia) and MCF7 (breast adenocarcinoma) human cancer cell lines. Values of IC50 (drug concentrations lethal for 50% of the tumour cells) ranged from 4.5 to 14.1 μm for the K-562 cells and from 4.3 to 21.0 μm for the MCF7 cells. The in vitro cytotoxicities were in several cases comparable or even higher than those of therapeutically used platinumbased anticancer drugs, that is, cisplatin, carboplatin and oxaliplatin.
