1,721,025 research outputs found
Identification of genes associated with platinum iminoether compounds activity in ovarian cancer cells
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Platinum(II)-Acyclovir complexes of acyclovir: synthesis, antiviral and antitumor activity
No full textA platinum(II) complex with the antiviral drug acyclovir was synthesized and its
antiviral and anticancer properties were investigated in comparison to those of acyclovir and
cisplatin. The platinum-acyclovir complex maintained the antiviral activity of the parent
drug acyclovir, though showing a minor efficacy on a molar basis (IDs0 7.85 and 1.02 laM
for platinum-acyclovir and cisplatin, respectively). As anticancer agent, the platinumacyclovir
complex was markedly less potent than cisplatin on a mole-equivalent basis, but it
was as effective as cisplatin when equitoxic dosages were administered in vivo to P388
leukaemia-bearing mice (%T/C 209 and 211 for platinum-acyclovir and cisplatin,
respectively). The platinum-acyclovir complex was also active against a cisplatin-resistant
subline of the P388 leukaemia (%T/C 140), thus suggesting a different mechanism of
action. The DNA interaction properties (sequence specificity and interstrand cross-linking
ability) of platinum-acyclovir were also investigated in comparison to those of cisplatin and
[Pt(dien)C1]+, an antitumour-inactive platinum-triamine compound. The results of this study
point to a potential new drug endowed, at the same time, with antiviral and anticancer
activity and characterized by DNA interaction properties different from those of cisplatin
Differential processing of antitumour-active and antitumour-inactive trans platinum compounds by SKOV-3 ovarian cancer cells
Full text linkIn order to compare the mechanistic properties of the antitumour-active trans platinum complex trans-[PtCl2{Z-HN = C(OMe)Me}(NH3)] (trans-Z) and of the antitumour-inactive isomer of cisplatin tTanS-[PtCl2(NH3)(2)] (trans-DDP), the differential processing of the two compounds by SKOV-3 ovarian cancer cells has been investigated. trans-Z and trans-DDP enter cells with the same efficacy, but trans-Z shows a two-fold higher affinity for cellular DNA. The treatment with trans-DDP IC50 determines an initial and transient cytostatic effect, paralleled by a moderate increase of apoptosis and by sequential and reversible arrests in S and G(2)/M phases of cell-cycle. In contrast, trans=Z IC50 determines an initial cytotoxic effect, a more persistent and marked increase of apoptosis, and a more marked and prolonged arrest in S and G(2)/M phases of the cell-cycle. Treatment-induced gene expression modifications indicate that phenotypic effects of trans-DDP are driven by an initial and transient up-regulation of some genes related to cell-cycle checkpoint and arrest networks, whereas the more dramatic phenotypic effects of trans-Z are driven by a persistent up-regulation of more numerous genes involved in cell-cycle checkpoint and arrest networks, and in genome stability and DNA repair. Therefore, molecular and cellular events have been identified which are produced by trans-Z but not by trans-DDP, and which likely represent the mechanistic basis of antitumour activity of trans-Z in the SKOV-3 system. (c) 2006 Elsevier Inc. All rights reserved
In vitro antitumor activity of 2-acetyl pyridine 4n-ethyl thiosemicarbazone and its platinum(II) and palladium(II) complexes
No full textThe reaction of platinum(II) [Pt(II)] or palladium(II) [Pd(II)]
with 2-acetyl pyridine 4N-ethyl thiosemicarbazone,
HAc4Et (1) results in the complexes [Pt(Ac4Et) 2 ] (2) and
[Pd(Ac4Et) 2 ] (3). In a panel of human tumor cell lines of
different origins (breast, colon, and ovary cancers), and
containing also cisplatin-refractory/resistant cell lines,
the in vitro growth inhibitory effect of 1–3 was compared
to that of cisplatin by using the sulforodamine B assay.
After a 96-hour continuous treatment, both the thiosemicarbazone
HAc4Et and the metal compounds [Pt(Ac4Et) 2 ]
and [Pd(Ac4Et) 2 ] exhibit very remarkable growth inhibitory
activities with mean IC 50 values of 0.9 n M (0.22–
2.47 n M ), 0.7 n M (0.15–2 n M ) and 0.5 n M (0.17–1.02 n M ),
respectively. In contrast, cisplatin shows a markedly lower
growth inhibitory potency, the mean IC 50 in the panel
being 2.8 _ M (0.2–8 _ M ). In addition to their major cell
growth inhibitory potency, complexes 1–3 are characterized
by a growth inhibitory profi le different from that of
cisplatin, being active towards cisplatin-refractory tumor
cell lines. These fi ndings, along with the ability of completely
overcoming acquired cisplatin resistance from
either multifocal or reduced uptake origin, confi rm the
antitumor potential of HAc4Et and support the hypothesis
that both [Pt(Ac4Et) 2 ] and [Pd(Ac4Et) 2 ] complexes
can be characterized by cellular pharmacological properties
distinctly different from those of cisplati
Platinum complexes with bisphosphonate analogue: a novel dual mechanism of antitumour action
No full textGenomic analysis of the differential processing of antitumor-active and antitumor-inactive trans platinum compuonds
No full textProcesso di sintesi di complessi di platino con imminoeteri e loro utilizzazione come agenti antitumorali e agenti modificanti le basi nucleotidiche
No full textMethod for synthesizing complexes of platinum with iminoethers and their use as antitumoral drugs and nucleotide base modifiers
No full textMMP activity inhibition by platinum-diethyl[(methylsulfinyl)methyl]phosphonate (SMP) complexes”
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