A Study on Synthesis of Novel Tetrandrie Deriatives and Their Antitumor Activity
This study designs and synthesizes tetrandrine derivatives and investigates their anti-tumor activity.The key intermediate 5-bromotetrandrine was synthesized from tetrandrine by bromination,and then exchanged with lithium bromide to form lithium salt.Eight new tetrandrine derivatives were synthesized by the addition of aro-matic aldehydes.Their structures were confirmed by 1HNMR,13CNMR,and ESI-MS.MTT assay was used to evalu-ate the antitumor activities of eight samples against HepG2 and human BGC-823.The preliminary screening results showed that compound 2 had the strongest inhibition on HepG2 cells and compound 1 had the strongest inhibition on BGC-823 cells.Through structural modification,the antitumor activity of derivatives 1 and 2 of tetrandrine is grea-ter than that of tetrandrine.
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