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天然存在的倍半萜内酯类结构的物质具有显著的细胞毒抗肿瘤活性,例如双功能烷基化的堆心菊内酯(Helenalin),因其含有一个β-未取代环(?)烷和一个α-亚甲基-γ内酯,它的体外细胞毒性以及体内抗肿瘤活性比相应的2,3-二氢堆心菊内酯或11,13-二氢堆心菊内酯强得多。对堆心菊内酯以及有关的衍生物引进一个亲脂的酯侧链也能增强其细胞毒作用。上述表明,该类化合物的活性与它们的双功能烷基的enone 0=C-C=CH_2系统以及酯链有关。为此,作者对合成的堆心菊内酯,鸦胆子苦醇酯(Brusatol酯),鸦胆子丁
Naturally occurring substances of the sesquiterpenoid structure possess significant cytotoxic antitumor activity, such as bifunctional alkylated Helenalin, which contains a beta-unsubstituted cyclo And an alpha-methylene-gamma lactone, which have in vitro cytotoxicity and in vivo antitumor activity stronger than the corresponding 2,3-dihydro-d-galactone or 11,13- many. The introduction of a lipophilic ester side chain to hesperetin and related derivatives also enhances its cytotoxicity. The above shows that the activity of these compounds is related to the enone 0 = C-C = CH 2 system of their bifunctional alkyl groups and the ester chain. To this end, the author of the synthetic hesperetin, Brucein ester (Brusatol ester), brucei d