Mimicry of annonaceous acetogenins:: Enantioselective synthesis of a (4R)-hydroxy analogue having potent antitumor activity
Mimicry of annonaceous acetogenins:: Enantioselective synthesis of a (4R)-hydroxy analogue having potent antitumor activity
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DOI：
10.1021/jo016396u
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发表时间：
2002-05-17
影响因子：
3.6
通讯作者：
Yao, ZJ
中科院分区：
文献类型：
--
作者：
Jiang, S;Liu, ZH;Yao, ZJ
番荔枝内酯的（4 R）-羟基化类似物模拟化合物2是在天然存在的番荔枝内酯bullatacin的结构基础上设计和合成的，bullatacin被发现是具有强细胞毒性、抗肿瘤和其他生物活性的新型聚酮化合物家族的典型成员。初步筛选显示，2对HT-29和HCT-8的IC 50值分别为1.6 x 10（-3）和8 x 10（-2）μ g/mL。通过对1c及其（4 R）羟基化类似物2的活性比较，观察到了显著的增强效应。
The (4R)-hydroxylated analogues of annonaceous acetogenin mimicking compound 2 were designed and synthesized structurally on the basis of the naturally occurring annonaceous acetogenin bullatacin, which was discovered as a typical member of the novel family of polyketides with potent cytotoxicity, antitumoral, and other biological activities. The preliminary screenings show that the IC50 values of 2 were 1.6 x 10(-3) and 8 x 10(-2) mug/mL against HT-29 and HCT-8, respectively. A remarkable enhancement effect was observed by the activity comparison of 1c and its (4R)hydroxylated analogue 2.