Von Angerer, Erwin and Knebel, Norbert and Schönenberger, Helmut and Engel, Juergen (1988) Preparation of aminoplatinum phenylindole antitumor agents.
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Abstract
Title compds. I (X = physiolog. acceptable anion; R1 = H, OH, C2-6 alkamoyloxy; R2 = H, halo; R3 = H, C1-6 alkyl; R4 = OH, C2-6 alkamoyloxy; R5, R6 = H, halo; Alk = C2-10 alkylene with 1,4-phenylene optionally in chain; A-B = alkylenediamine, etc.) are prepd. as antitumor agents. Reaction of 1.01 mmol each of II and K2PtCl4 in DMF/H2O at 40 Deg for 24 with exclusion of light gave III. I showed .apprx.89% control of hormone-dependent breast cancer at 20 mg/kg s.c. in mice and rats. Tablet and injection formulations are given.
| Item Type: | Patent | ||||||
|---|---|---|---|---|---|---|---|
| Additional information (public): | CAN 109:47368 78-7 Inorganic Chemicals and Reactions Patent 19880406 91444-18-7 Role: RCT (Reactant), RACT (Reactant or reagent) (alkylation of); 629-03-8 (1,6-Dibromohexane) Role: RCT (Reactant), RACT (Reactant or reagent) (alkylation of phenylindole deriv. by); 115140-97-1P; 115140-98-2P; 115140-99-3P; 115141-00-9P; 115141-01-0P; 115141-02-1P; 115160-74-2P; 115160-75-3P; 115357-82-9P; 115357-83-0P; 115357-84-1P; 115357-85-2P; 115357-86-3P; 115357-87-4P; 115357-88-5P; 115357-89-6P; 115357-90-9P; 115362-88-4P; 115378-88-6P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of, as antitumor agent); 115084-37-2P; 115084-38-3P; 115084-40-7P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of, as intermediate for phenylindolealkyleneamino ligand); 115084-39-4P; 115084-41-8P; 115084-42-9P; 115084-43-0P Role: SPN (Synthetic preparation), PREP (Preparation) (prepn. of, as ligand for aminoplatinum antitumor agent); 1121-60-4 (2-Pyridinealdehyde) Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with aminohexylphenylindole deriv.); 107-15-3 (1,2-Ethanediamine) Role: RCT (Reactant), RACT (Reactant or reagent) (reaction of, with methoxyphenylindole deriv.) Designated States R: AT, BE, CH, DE, ES, FR, GB, GR, IT, LI, LU, NL, SE. A2 DE 86-3633673 19861003 | ||||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger | ||||||
| Projects: | SFB 234 | ||||||
| Identification Number: |
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| Keywords: | Neoplasm inhibitors (platinum phenylindolealkyleneamino complexes) platinum phenylindolealkyleneamine complex prepn antitumor | ||||||
| Subjects: | 500 Science > 540 Chemistry & allied sciences | ||||||
| Status: | Published | ||||||
| Refereed: | Yes, this version has been refereed | ||||||
| Created at the University of Regensburg: | Yes | ||||||
| Owner: | Petra Gürster | ||||||
| Deposited On: | 15 Nov 2010 16:34 | ||||||
| Last Modified: | 15 Nov 2010 16:34 | ||||||
| Item ID: | 18063 |
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