Synthesis, characterization, and antitumor activity of a series of novel cisplatin analogs with cis-1,4-diaminocyclohexane as nonleaving amine group

被引:48
作者
Shamsuddin, S [1 ]
Takahashi, I [1 ]
Siddik, ZH [1 ]
Khokhar, AR [1 ]
机构
[1] UNIV TEXAS,MD ANDERSON CANC CTR,DEPT CLIN INVEST,HOUSTON,TX 77030
关键词
D O I
10.1016/0162-0134(95)00084-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of novel platinum(II) complexes of the type Pt-II(cis-1,4-DACH)X (where cis-1,4-DACH = cis-1,4-diaminocyclohexane and X = dichloro, sulfate, oxalato, malonato, methylmalonato, tartronato, or 1,1-cyclobutanedicarboxylato [CBDCA) ligand and novel platinum(IV) complexes of the types Pt-IV(cis-1,4-DACH)trans(Y)(2)Cl-2 (where Y = chloro, hydroxo, acetato, propionato, or butyrato ligand) and Pt-IV(cis-1,4-DACH)trans(Cl)(2)(X) (where X = oxalato or CBDCA ligand) were synthesized and characterized by elemental analysis, infrared, and Pt-195 NMR spectroscopic techniques. Platinum complexes had good in vitro cytotoxic activity against murine leukemia L1210/0 (IC50 = 0.0032 - 1.60 mu M) and human ovarian A2780 (IC50 = 0.045 - 0.430 mu M) cell lines.
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页码:291 / 301
页数:11
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