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J Pharm Sci ; 82(9): 927-33, 1993 Sep.
Article in English | MEDLINE | ID: mdl-8229691

ABSTRACT

A synthetic design was devised for preparing primary amines related to anticancer drugs clomiphene and tamoxifen on the basis of key intermediates with a phenolic group, to which a side chain (omega-aminoethoxy or omega-aminopropoxy) was attached. These compounds were then reacted with 2,4,6-trimethyl- or 2,4,6-triphenylpyrylium salts. This afforded pyridinium analogues of clomiphene and tamoxifen as potential therapeutic agents for treatment against hormone-dependent tumors.


Subject(s)
Antineoplastic Agents/chemical synthesis , Pyrans/chemical synthesis , Pyridinium Compounds/chemical synthesis , Antineoplastic Agents/pharmacology , Clomiphene/analogs & derivatives , Drug Screening Assays, Antitumor , Humans , Magnetic Resonance Spectroscopy , Neoplasms, Hormone-Dependent/drug therapy , Pyrans/pharmacology , Pyridinium Compounds/pharmacology , Tamoxifen/analogs & derivatives , Tumor Cells, Cultured
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