Water-soluble third generation antitumor platinum complexes, [2,2-bis(aminomethyl)-1,3-propanediol-N,N']-[1,1-cyclobutanedicarboxylato(2-)-O,O']platinum(II) and [1,1-cyclobutanedicarboxylato(2-)-O,O'][tetrahydro-4H-pyran-4,4-dimethanamine-N,N']platinum(II)

The synthesis, stability, and antitumor activity of a series of water-soluble third generation platinum(II) complexes have been described. Among these complexes, [2,2-bis(aminomethyl)-1,3- propanediol-N,N'] [1,1-cyclobutanedicarboxylato(2-)-O,O']platinum(II) and [1,1-cyclobutanedicarboxyla...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1989-08, Vol.32 (8), p.2015-2020
Main Authors: Bitha, Panayota, Carvajal, Suzanne G, Citarella, Ronald V, Child, Ralph G, Delos Santos, Eugenia F, Dunne, Theresa S, Durr, Fredrick E, Hlavka, Joseph J, Lang, S. A
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - therapeutic use
Bioinorganic chemistry
Carboplatin - analogs & derivatives
Chemical Phenomena
Chemistry
Exact sciences and technology
Female
Humans
Inorganic chemistry and origins of life
Mice
Mice, Nude
Models, Molecular
Neoplasm Transplantation
Neoplasms, Experimental - drug therapy
Organoplatinum Compounds - chemical synthesis
Organoplatinum Compounds - therapeutic use
Structure-Activity Relationship
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Summary:The synthesis, stability, and antitumor activity of a series of water-soluble third generation platinum(II) complexes have been described. Among these complexes, [2,2-bis(aminomethyl)-1,3- propanediol-N,N'] [1,1-cyclobutanedicarboxylato(2-)-O,O']platinum(II) and [1,1-cyclobutanedicarboxylate(2-)-O,O'](tetrahydro-4H-pyran-4,4- dimethanamine-N,N'-)platinum(II) have shown the greatest promise for further investigation and are currently under clinical evaluation.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00128a052