Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents

A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde.  Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay.  It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization.  The results also indicated that the potency of compound 31 is about three times more than that of noscapine against HL-60 cell line and tubulin polymerization.  Moreover, it induced a massive accumulation of cells in G₂/M phase.  These results showed noscapine and its derivatives were worth to be intensively studied further.