[CITATION][C] Platinum complexes in cancer chemotherapy

M Rozencweig, DD Von Hoff, R Catane… - Fundamentals in Cancer …, 1978 - karger.com
M Rozencweig, DD Von Hoff, R Catane, FM Muggia
Fundamentals in Cancer Chemotherapy, 1978karger.com
Structurally, DDP shows a square planar geometry. Most of the platinum derivatives that
have been subsequently synthetized share a common general formula of the type Pt A2 X2.
Generally, the trans-isomers are inactive in animal tumor models although they may exhibit
significant toxicity [6]. Successful substitutions of the X components have used monodentate
anionic ligands of intermediate leaving ability, mainly chlorides, or bidentate ligands such as
sulfate or malonate; most of the A components have been mono-or bidentate aliphatic …
Structurally, DDP shows a square planar geometry. Most of the platinum derivatives that have been subsequently synthetized share a common general formula of the type Pt A2 X2. Generally, the trans-isomers are inactive in animal tumor models although they may exhibit significant toxicity [6]. Successful substitutions of the X components have used monodentate anionic ligands of intermediate leaving ability, mainly chlorides, or bidentate ligands such as sulfate or malonate; most of the A components have been mono-or bidentate aliphatic, aromatic and heterocyclic amine ligands [6, 7, 61]. The yield of these syntheses has been generally deceptive; only a few of these newer compounds have demonstrated a minimal improvement in therapeutic index over DDP and some have undergone or are currently undergoing exploratory clinical trials (25, 35]. Platinum pyrimidine blues form a separate group of platinum complexes of still undefined structure [11]. They result from the reaction of the diaquo species of DDP and pyrimidines or substituted pyrimidines. They are characterized by a high degree of water solubility and show significant antitumor properties in animal models with much lesser kidney damage as
Karger