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@article{837777,
author = {RamosandLima, Francisco J. and Vrána, Oldřich and Quiroga, Adoración G. and NavarroandRanninger, Carmen and Halámiková, Anna and Rybníčková, Hana and Hejmalová, Lenka and Brabec, Viktor},
article_location = {USA},
article_number = {8},
keywords = {transplatin; antitumor; DNA},
language = {eng},
issn = {0022-2623},
journal = {Journal of Medicinal Chemistry},
title = {Structural Characterization, DNA Interactions, and Cytotoxicity of New Transplatin Analogues Containing One Aliphatic and One Planar Heterocyclic Amine Ligand},
volume = {49},
year = {2006}
}
TY - JOUR
ID - 837777
AU - Ramos-Lima, Francisco J. - Vrána, Oldřich - Quiroga, Adoración G. - Navarro-Ranninger, Carmen - Halámiková, Anna - Rybníčková, Hana - Hejmalová, Lenka - Brabec, Viktor
PY - 2006
TI - Structural Characterization, DNA Interactions, and Cytotoxicity of New Transplatin Analogues Containing One Aliphatic and One Planar Heterocyclic Amine Ligand
JF - Journal of Medicinal Chemistry
VL - 49
IS - 8
SP - 2640-2651
EP - 2640-2651
PB - American Chemical Society
SN - 00222623
KW - transplatin
KW - antitumor
KW - DNA
N2 - We report in the present work new analogues of clinically ineffective transplatin in which one ammine group was replaced by aliphatic and the other by a planar heterocyclic ligand, namely trans-[PtCl(2)(isopropylamine)(3-(hydroxymethyl)-pyridine)], 1, and trans-[PtCl(2)(isopropylamine)(4-(hydroxymethyl)-pyridine)], 2. The new compounds, in comparison with parent transplatin, exhibit radically enhanced activity in tumor cell lines both sensitive and in particular resistant to cisplatin. Concomitantly, the DNA binding mode of 1 and 2 compared to parent transplatin and other antitumor analogues of transplatin in which only one ammine group was replaced is also different. The results also suggest that the reactions of glutathione and metallothionein-2 with compounds 1 and 2 do not play a crucial role in their overall biological effects. In addition, the monofunctional adducts of 1 and 2 are quenched by glutathione considerably less than the adducts of transplatin, which may potentiate cytotoxic effects of these new platinum complexes.
ER -
RAMOS-LIMA, Francisco J., Oldřich VRÁNA, Adoración G. QUIROGA, Carmen NAVARRO-RANNINGER, Anna HALÁMIKOVÁ, Hana RYBNÍČKOVÁ, Lenka HEJMALOVÁ and Viktor BRABEC. Structural Characterization, DNA Interactions, and Cytotoxicity of New Transplatin Analogues Containing One Aliphatic and One Planar Heterocyclic Amine Ligand. \textit{Journal of Medicinal Chemistry}. USA: American Chemical Society, 2006, vol.~49, No~8, p.~2640-2651. ISSN~0022-2623.
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