Abstract A series of 1-phenyl-3, 4-dihydroisoquinoline derivatives and several 1-phenyl-1, 2, 3, 4-tetrahydroisoquinoline, 1-phenyl-isoquinoline analogues were synthesized, and their cytotoxicity and tubulin polymerization inhibitory activity were evaluated. The 1-phenyl-3, 4- dihydroisoquinoline compounds were found to be potential tubulin polymerization inhibitors. Compound 5n, bearing a 3′[BOND] OH and 4′[BOND] OCH 3 substituted 1-phenyl B- ...