Cis-platinum (II) complexes wherein platinum (II) coordinates 1,2-diamino-cyclohexane (cis-, trans-l-or trans-d-) are disclosed. The complexes exhibit anti-tumor activity.
Unique, valuable and multifariously utile macromolecular complexes are comprised of: (i) non-ionic, amidocarbonylic, water-soluble polymers (and, for some embodimental purposes, the monomeric precursor(s) thereof), including such known materials as (poly)N-vinylpyrrolidone (i.e., "PVP") and/or (poly)N-vinyl-5-methyl-2-oxazolidinone (i.e., "PVO-M") and the hereinafter disclosed like(s) and/or equivalent(s) thereof which, for convenience, may be herein generically identified as "WSP"; and (ii) square planar configured platinous and, for instant applicancy, equivalently metalled organometallic compounds characterized in containing in ligandal inclusion an aromatic moiety from which depends and to which is connected at least a single distinctly polar substituent group (or "handle", as it were), such as an hydroxide (i.e., "--OH"), carboxylic acid (i.e., "--COOH") or sulfonic acid - (i.e., "--SO.sub.3 H") unit and/or equivalents thereof as herein disclosed which, for convenience, may for generic identification be herein called an "SPOM". The WSP:SPOM complex(es) are associated by non-ionic or other bonding attachment in the nature of hydrogen bonding and/or closely related electrostatic interaction between or through and to the polar substituent in the SPOM and the amidocarbonylic unit in the WSP.
Disclosed herein are novel complex compounds of platinum showing an antitumor activity, represented by the formula(I): ##STR1## wherein one of R.sup.1 and R.sup.2 represents a group selected from the group consisting of (1) glucuronato groups whose hydroxyl groups may be acylated, (2) gluconato groups whose hydroxyl groups may be acylated, (3) pyruvato group and (4) nitrato group, and the other of R.sup.1 and R.sup.2 represents a group selected from the group consisting of (i) glucuronato groups whose hydroxyl groups may be acylated, (ii) gluconato groups whose hydroxyl groups may be acylated, (iii) pyruvato group and (iv) halogen atoms, or R.sup.1 and R.sup.2 represent together the group represented by the formula(II): ##STR2##
Novel platinum(II) complexes of 1,2-diaminocyclohexane, 2,2'-bipiperidine, 1,2-diamino-2,4-dimethylpentane, 1,2-diaminocyclooctane, 3,4-diamino-2,5-dimethylhexane and 1-aminomethylcyclooctylamine are provided: such complexes are of use in inhibiting the growth of certain mammalian tumors.
Organo-platinum complexes of the following formula having excellent antitumor actions: ##STR1## X and Y each or taken together is a mono- or bi-functional ligand selected from the group consisting of halogeno, nitrato, sulfonato, monocarboxylato (mono-functional), sulfato, and dicarboxylato (bi-functional); and each of n and m is an integer of 1 or 2.
1,2-Diaminocyclohexane platinum (II) complexes of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, are selected from nitrate and various organic carboxylate groups, with the proviso that R.sub.1 and R.sub.2 are not both nitrate, and the configuration of the 1,2-diaminocyclohexane being selected from cis, trans-d and trans-1, have been found to exhibit potent cytostatic activity. They may be made by reacting a starting material, in which R.sub.1 and R.sub.2 are nitrate, with the appropriate carboxylic acid or salt thereof.