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本文制备了3α-溴-表苦鬼臼脂素,首次在鬼臼脂素结构修饰中在C环3-位引入取代基。其体外抑制KB细胞和L1210白血病细胞活性均高于阳性对照药。在碱性条件下,其可被方便地转化为4β-羟基-2,3-不饱和苦鬼臼脂素,进而2,3-不饱和鬼臼脂素衍生物可被合成。由于具有较好的体外抑制肿瘤细胞活性,该化合物可作为结构修饰的先导化合物。由于3-位溴原子的引入,其又是鬼臼脂素类化合物结构转化的中间体。
In this paper, 3α-bromo-epipodophyllotoxin was prepared and introduced into the 3-position of the C ring for the first time in the structural modification of podophytonin. Its in vitro inhibition of KB cells and L1210 leukemia cells were higher than the positive control activity. Under basic conditions, it can be conveniently converted to 4β-hydroxy-2,3-unsaturated pipodophyllotoxin, which in turn can be synthesized as a 2,3-unsaturated podophyllotoxin derivative. Due to its good activity of inhibiting tumor cells in vitro, the compound can be used as a structural modification lead compound. Due to the introduction of the 3-position bromine atom, it is also an intermediate for the structural transformation of podophyllotoxin compounds.