Platinum-amine complexes activity

STRUCTURE-ACTIVITY RELATIONSHIPS OF PLATINUM-AMINE COMPLEXES... 

The original finding of the antibacterial activity of platinum—amine complexes led, of course, to the discovery of their antitumour activity [40]. The initial electrolysis product from the platinum electrode in Rosenberg s initial experiment was the hexachloroplatinate(IV) species, [PtCl ]... 

Since platinum(IV) complexes are also kinetically inert, optical diastereomers of Pt(en)2(L-2,3-diaminopropionic acid)4+ have been prepared.1028 The first synthetic procedure involves the chlorine oxidation of PtCl2(L-2,3-diaminopropionic acid) followed by reaction with ethylenedi-amine. Resolution is achieved through the (+)-tartrate salt. Alternatively the resolved complex can be prepared directly from the reaction of L-2,3-diaminopropionic acid on optically active cis-[PtCl2(en)2]Cl2. (... 

Bis(phosphoranimine) ligands, chromium complexes, 5, 359 Bis(pinacolato)diboranes activated alkene additions, 10, 731—732 for alkyl group functionalization, 10, 110 alkyne additions, 10, 728 allene additions, 10, 730 carbenoid additions, 10, 733 diazoalkane additions, 10, 733 imine additions, 10, 733 methylenecyclopropane additions, 10, 733 Bisporphyrins, in organometallic synthesis, 1, 71 Bis(pyrazol-l-yl)borane acetyl complexes, with iron, 6, 88 Bis(pyrazolyl)borates, in platinum(II) complexes, 8, 503 Bispyrazolyl-methane rhodium complex, preparation, 7, 185 Bis(pyrazolyl)methanes, in platinum(II) complexes, 8, 503 Bis(3-pyrazolyl)nickel complexes, preparation, 8, 80-81 Bis(2-pyridyl)amines... 

We certainly do not intend these rules to restrict future research, but only to encompass a large amount of past experience with platinum(II) complexes. Obviously exceptions will, and have already, occurred. For example, the high activity of bidentate leaving groups such as oxalate and malo-nate (see structures of Fig. 4) first synthesized by M. Cleare and J. Hoe-schele in this laboratory are not encompassed nor is the effect of cyclic amines, developed by Tobe, which decrease the solubility of the complexes, but markedly enhance the antitumor activity. Here, studies of the rela-... 

Swiss pharmaceutical company Roche. It is a new platinum anticancer drug, result of a trinuclear platinum coordination complex with chloride and amine ligands. It is active through covalent adducts with DNA inducing apoptosis. 

Distribution measurements show that the silver complex of dr-cyclo-octene is less stable than that of cycloheptene, presumably owing to more ring strain in the latter 129,130). tronr-Cyclooctene is considerably more strained than the cis isomer, and can be separated from it by extraction with 20% aqueous silver nitrate 32), but there are no quantitative measurements of the stability of the silver complex of the tram isomer. The interesting possibility of isomerizing cis to trom-cyclooctene via metal complexes has not yet been achieved. tronr-Cyclooctene has been resolved via its platinum(II) complex with the optically active amine l-phenyl-2-amino-propane (am), 7r-CgH]4PtCl2am. 29). 

Current interest in the use of metal complexes for the treatment of cancer was triggered by the discovery of the anticancer activity of Pt(ll) amine complexes in 1969 by Rosenberg [10]. Now at least four platinum complexes have been approved for clinical use (complexes 1-4, Fig. 2.1) and platinum complexes are the most widely-used anticancer drugs. Stimulation for the discovery of anticancer complexes of metals other than platinum arises from the cellular resistance to platinum which is sometimes encountered in the clinic, the toxic side-effects of dsplatin (1), which can be severe, and the limited spectrum of activity against different types of cancer [11]. 

Feiruti, P., Ranucci, E., Trotta, F., Gianasi, E., Evagorou, E. G., Wasil, M., Wilson, G., Duncan, R., 1999, Synthesis, characterization, and antitumor activity of platinum(II) complexes of novel functionalised polytamido amine)s. Macromol. Chem. Phys. 200 1644-1654. 

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