Platinum polyamines biological activity

This paper presents preliminary biological assay results related to potential antineoplastic activity for select platinum polyamines of Form IV. 

PLATINUM II POLYAMINES DETERMINATION OF SIZE, DEGRADATION AND BIOLOGICAL ACTIVITY... 

Which of these four potential advantages, if any, actually occurs with the platinum polymers is currently being studied. Approximately two dozen platinum polyamines have been synthesized, and some show biological activity while others do not (126-128). Several of the polymers properties are being explored and correlated with polymer activity in an effort to discover why certain polymers are active while others are inactive. Such factors as the nature of the diamine component, the extent to which a polymer is transported into the cell, the rate of aquation, etc., could all influence the biological activity of a polymer. Two other properties that could control polymer activity are the size of a polymer and the tendency of a polymer to degrade, and these will be the subject of discussion here. 

The biological activity of the platinum polyamines was tested in cell culture using two cell lines derived from mouse fibroblasts. Balb/3T3 cells resemble normal cells in their growth properties m-MSV Balb/3T3 cells have been transformed and resemble cancer cells in their growth properties. 

We recently reported the synthesis of polymeric platinum II derivatives of cis-dichlorodiamineplatinum II, cis-DDP (2 1,2). These polyamines (2) exhibit good inhibition towards a wide range of tumor cells including L929, WISH and HeLa cell lines with good cell differentiation. Some extend the life of (induced) terminally ill cancerous mice by 50%. Further the polyamines exhibit activity towards virus at concentration levels where the cells are unaffected. Recent biological studies are aimed at evaluation of certain polyamines on inhibiting select tumors and viruses for specific disease control. 

The present volume is the fourth in the series and covers the topics lithium in biology, the structure and function of ceruloplasmin, rhenium complexes in nuclear medicine, the anti-HIV activity of macrocyclic polyamines and their metal complexes, platinum anticancer dmgs, and functional model complexes for dinuclear phosphoesterase enzymes. The production of this volume has been overshadowed by a very sad event—the passing away of the senior editor, Professor Robert W. Hay. It was he who conceived the idea of producing this series and who more than anyone else has been responsible for its continuation. A tribute by one of his many friends, Dr. David Richens, is included in this Volume. 

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