Diamine platinum complexes as antitumor agents

Details Diamine platinum complexes as antitumor agents Diamine platinum complexes as antitumor agents

1994-09-30

1995-07-18

Prescott, Arthur C.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heavy metal containing

C07F 1500, A61K 31555

Patent

active

054342562

ABSTRACT:
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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