Synthesis and Biological Evaluation of 7-Hydroxy-3,4-diphenyl-1,2-dihydroisoquinolines as New 4-Hydroxytamoxifen Analogues

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A phenolic 3,4-diphenyl-1,2-dihydroisoquinoline derivative (4a) as a new 4-hydroxytamoxifen analogue and a related compound (4c) were synthesized from 3,4-diphenyl-1,2,3,4-tetrahydroisoquinolin-ols (5a, c), which were prepared by intramolecular Barbier reaction of N-(2-iodobenzyl)phenacylamines. Anti-proliferative activities of 4a, c and 5a, c, as well as 4b and 5b prepared previously, against human mammary carcinoma MCF-7 cell line and human nasopharyngeal carcinoma KB cell line were evaluated. The 3,4-diphenyl-1,2-dihydroisoquinoline derivatives (4a, c) and isoquinolin-4-ols (5a, b) were active against MCF-7 cells and were nearly equipotent to the corresponding nonphenolic compound (1a). The mechanism of the anti-proliferative activity of 4a-c against MCF-7 cells is discussed.
公益社団法人日本薬学会の論文
1997-05-15