1.Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents.
Houling DAI ; Jianbin ZHENG ; Min LIN ; Jing ZHENG ; Fusheng ZHOU ; Xiaochun DONG ; Lei GUO ; Jianwen LIU ; Ren WEN
Acta Pharmaceutica Sinica 2012;47(10):1347-57
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 ofnoscapine 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.
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