Schönenberger, Helmut and Bissinger, Herbert and Thiel, Gerhard and Zippel, Horst and Beck, Wolfgang (1983) cis-Dichloroamino acid platinum(II) complexes.
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Cytostatic Cl2Pt(NH2CHRCO2R1)2 (I) (R = H or a group derived from biol. acceptable amino acids and R1 = C>2 alkyl or hydroxy-substituted group) with low toxicity and a strong antitumor effect are prepd. by reaction of II with alcs. (R1OH) and HCl or by treatment of K2PtCl4 with amino acid ester hydrochlorides. The in vitro ED50 of I (R = H, R1 = Et) [82474-52-0], I (R = H, R1 = Bu) [82474-53-1], and I (R = H, R1 = tert-Bu) [82474-54-2] against hormone-dependent human MDA-MB 231 mammary carcinoma cell culture were 1.0 * 10-5, 2.8 * 10-6, and 5.0 * 10-6M, resp. These complexes were as active as the free carboxylic acid contg. complexes, cis-PtCl2(NH2CHRCO2H)2.
|Additional information (public):||CAN 99:33119 1-6 Pharmacology Patent 19830203 82474-52-0P; 82474-53-1P; 82474-54-2P; 82474-55-3P; 82474-56-4P; 86293-63-2P Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses) (prepn. and antitumor activity of); 14592-69-9 Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with alcs. and hydrochloric acid, cis-platinum complexes from); 10025-99-7 Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with amino acid esters) A1|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Amino acids Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), BIOL (Biological study) (alkyl esters, dichloroplatinum complexes, prepn. and antitumor activity of) Cytotoxic agents Neoplasm inhibitors (dichloro(amino acid)platinum complexes) Alcohols Role: RCT (Reactant), RACT (Reactant or reagent) (aliph., reaction of, with amino acid platinum complexes in hydrochloric acid presence) chloro amino acid platinum cytostatic|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||15 Nov 2010 15:01|
|Last Modified:||15 Nov 2010 15:01|