Binuclear Pyrazoles. I. Synthesis and Cytotoxic Activity of 1,1'-Dibenzyl and 1,1'-Dihydroxymethyl 4,4'-Bispyrazoles

概要

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From 3,3', 5,5'-tetramethyl-4,4'-bis-1 H-pyrazole, 3,3', 5,5'-tetramethyl-4,4'-methylenebis-1 H-pyrazole and 4,4'-methylenebis-1 H-pyrazole, the corresponding 1,1'-dibenzyl and 1,1'-dihydroxymethyl derivatives have been obtained. Benzylation of 1H-bispyrazoles was carried out by treatment with benzyl chloride under phase transfer conditions. Hydroxymethylation was done by treatment with 37% aqueous formaldehyde either in acidic or in neutral medium. All the products obtained have been evaluated as cytotoxic, and 1,1'-dibenzyl-3,3', 5,5'-tetramethyl-4,4'-bispyrazole is a powerful cytotoxic agent (ED_<50>=7 μM).
社団法人日本薬学会の論文
1985-06-25