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 ...