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1,2-Diphenylethylenediamine platinum complexes as antitumor agents

Schönenberger, Helmut and Von Angerer, Erwin and Karl, Johann and Jennerwein, Margaretha and Engel, Juergen (1986) 1,2-Diphenylethylenediamine platinum complexes as antitumor agents.

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Abstract

The title compds. I [R = (substituted) Ph; R1 = H, C1-6 alkyl; X = pharmaceutically acceptable anion], useful as antitumor agents, are prepd. by complexation of a 1,2-diphenylethylenediamine ligand by a Pt compd. Thus, 248 mg meso-1,2-bis(4-fluorophenyl)ethylenediamine in 50% aq. Me3COH was treated with 415 mg K2PtCl4 at 50-60 Deg with exclusion of light to give I (R = 4-FC6H4, R1 = H, X = Cl). I were effective antineoplastics, e.g. at 100-200 mg/kg orally in mice with P 388 leukemia. Tablets (120 mg) were formulated from I (R = 2,6-Cl2C6H2OH-4, R1 = H, X = Cl) 200, lactose 500, microcryst cellulose 360, corn starch 130, and Mg stearate 10 g.

Item Type:

Patent

Additional information (public):

CAN 106:138636 29-13 Organometallic and Organometalloidal Compounds Patent 19860828 456-49-5 (3-Fluoroanisole) Role: RCT (Reactant), RACT (Reactant or reagent) (bromination of); 50648-93-6; 105469-16-7 Role: RCT (Reactant), RACT (Reactant or reagent) (complexation of, by platinum); 105469-14-5 Role: RCT (Reactant), RACT (Reactant or reagent) (halogenation of); 33719-74-3 (3,5-Dichloroanisole) Role: RCT (Reactant), RACT (Reactant or reagent) (hydroxymethylation of); 400-72-6P (4-Bromo-3-trifluoromethylanisole); 402-07-3P (2-Bromo-5-trifluoromethylanisole); 450-88-4P (2-Bromo-5-fluoroanisole); 458-50-4P (4-Bromo-3-fluoroanisole) Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. and lithiation and formylation of); 86111-47-9P (2,6-Dichloro-4-methoxybenzyl alcohol) Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. and oxidn. of); 105855-87-6P; 105855-88-7P; 105856-09-5P; 105856-10-8P; 105856-11-9P; 105856-12-0P; 105856-13-1P; 105856-14-2P; 105856-15-3P; 105856-16-4P; 105856-17-5P; 105856-18-6P; 105856-19-7P; 105856-20-0P; 105856-21-1P; 105856-22-2P; 105856-23-3P; 105856-24-4P; 105856-25-5P; 105856-26-6P; 105856-27-7P; 105856-28-8P; 105856-29-9P; 105856-30-2P; 105856-32-4P; 105856-34-6P; 105856-36-8P; 105856-38-0P; 105869-49-6P; 105869-50-9P; 105928-12-9P; 105928-13-0P; 105928-14-1P; 105928-15-2P; 105928-16-3P; 105928-87-8P; 105990-36-1P; 105990-74-7P; 106400-42-4P; 125948-93-8P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn. of, as antitumor agent); 331-64-6P (2-Fluoro-4-methoxybenzaldehyde); 43192-31-0P (2-Bromo-4-methoxybenzaldehyde); 54439-75-7P; 82772-93-8P (2,6-Dichloro-4-methoxybenzaldehyde); 105469-13-4P (2-Iodo-4-methoxybenzaldehyde); 106312-36-1P (4-Methoxy-2-trifluoromethylbenzaldehyde) Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of, as intermediate in the synthesis of phenylethylenediamine ligands); 2186-92-7 (4-Methoxybenzaldehyde dimethylacetal) Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with butyllithium); 105469-15-6 Role: RCT (Reactant), RACT (Reactant or reagent) (redn. of) A1 DE 85-3506507 19850223

Institutions:

Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger

Projects:

SFB 234

Identification Number: