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)

P Bitha; S G Carvajal; R V Citarella; R G Child; E F Delos Santos; T S Dunne; F E Durr; J J Hlavka; S A Lang Jr; H L Lindsay

doi:10.1021/jm00128a052

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)

J Med Chem. 1989 Aug;32(8):2015-20. doi: 10.1021/jm00128a052.

Authors

P Bitha¹, S G Carvajal, R V Citarella, R G Child, E F Delos Santos, T S Dunne, F E Durr, J J Hlavka, S A Lang Jr, H L Lindsay, et al.

Affiliation

¹ American Cyanamid Company, Lederle Laboratories, Pearl River, New York 10965.

PMID: 2754720
DOI: 10.1021/jm00128a052

Abstract

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.

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / therapeutic use
Carboplatin* / analogs & derivatives*
Chemical Phenomena
Chemistry
Female
Humans
Mice
Mice, Nude
Models, Molecular
Neoplasm Transplantation
Neoplasms, Experimental / drug therapy
Organoplatinum Compounds / chemical synthesis*
Organoplatinum Compounds / therapeutic use
Structure-Activity Relationship

Substances

Antineoplastic Agents
Organoplatinum Compounds
zeniplatin
Carboplatin
enloplatin