发明授权
- 专利标题： Diamine platinum complexes as antitumor agents
- 专利标题（中）： 将铂络合物作为抗肿瘤剂二胺
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申请号： US316139申请日： 1994-09-30
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公开(公告)号： US5434256A公开(公告)日： 1995-07-18
- 发明人: Abdul R. Khokhar , Zahid H. Siddik
- 申请人： Abdul R. Khokhar , Zahid H. Siddik
- 申请人地址： TX Austin
- 专利权人： Board of Regents, The University of Texas System
- 当前专利权人： Board of Regents, The University of Texas System
- 当前专利权人地址： TX Austin
- 主分类号： C07F15/00
- IPC分类号： C07F15/00 ; A61K31/555
摘要：
Novel 1,4 and 1,2-diaminocyclohexane platinum IV complexes have been synthesized that show activity in vivo against tumor models resistant to cis-platin and tetraplatin. The novel complexes include the chloro, acetate, trifluoroacetate, propionate, butyrate, pentanoate, hexanoate and heptanoate as leaving ligands and 1,4 or 1,2-DACH-amine ligands. The complexes showed good in vitro cytotoxic activity against murine leukemia L1210/0, L1210/DDP and L1210/DACH. High in vivo activity was shown against L1210 leukemia cells and against cis-platin resistant L1210/DDP. Excellent antitumor activity against M5076 was also exhibited by the new complexes. Additionally, the platinum complexes did not elicit any indication of nephrotoxicity in the in vivo tests.
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