Platinum(IV) coordination compounds containing 5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one as nonleaving ligand. Molecular and cytotoxicity in vitro characterization

被引:12
|
作者
Lakomska, Iwona [1 ]
Fandzloch, Marzena [1 ]
Wojtczak, Andrzej [1 ]
Szlyk, Edward [1 ]
机构
[1] Nicolaus Copernicus Univ, Fac Chem, PL-87100 Torun, Poland
关键词
Platinum(IV) complex; 5-Methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one; NMR; X-ray structure; Cytotoxicity; X-RAY-STRUCTURE; ANTITUMOR-ACTIVITY; CRYSTAL-STRUCTURE; CARBOXYLATE COMPLEXES; ANTICANCER COMPLEXES; CELL-LINES; NMR; PALLADIUM(II); DNA; RESISTANCE;
D O I
10.1016/j.saa.2011.03.019
中图分类号
O433 [光谱学];
学科分类号
0703 ; 070302 ;
摘要
Novel platinum(IV) coordination compounds with 5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one (HmtpO): cis-trans-[PtCl2(OH)(2)(NH3)(HmtpO)] (1), cis-trans-[PtCl5(HmtpO)][(CH3)(2)NH2] (2) have been prepared and structurally characterized by spectroscopic methods (H-1, IR and X-ray crystallography (2)). The X-ray results indicate that the local geometry around the platinum(IV) centre approximates a typical octahedral arrangement with nitrogen atom N3 of the HmtpO and three chloride atoms in equatorial positions. The remaining two axial positions are occupied by two chlorides. The preliminary assessment of antitumor properties of (1) was performed as an in vitro antiproliferative activity against HL-60 human acute promyelocytic leukemia and HCV29T bladder cancer. The cis-trans-[PtCl2(OH)(2)(NH3)(HmtpO)] (1) exhibits higher cytotoxic activity against HL-60 (IC50=6.4 mu M) than cisplatin. (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:497 / 501
页数:5
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