SELECTIVE ALKYLATION - BIOMIMETIC REACTION OF ANTILEUKEMIC TRIPTOLIDES
SELECTIVE ALKYLATION - BIOMIMETIC REACTION OF ANTILEUKEMIC TRIPTOLIDES
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DOI：
10.1126/science.185.4153.791
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发表时间：
1974-01-01
期刊：
影响因子：
56.9
通讯作者：
SCHUBERT, RM
中科院分区：
文献类型：
--
作者：
KUPCHAN, SM;SCHUBERT, RM
有效的抗白血病植物成分雷公藤甲素和雷公藤内酯含有一个特有的氢键9，11-环氧基-14β-羟基体系。他们在一个过程中使丙硫醇烷基化，该过程涉及在邻近羟基的帮助下打开环氧化物功能。该反应可能通过与生长调节相关的关键酶的硫醇基团的选择性烷基化来模拟抑制肿瘤生长。
The potent antileukemic plant principles triptolide and tripdiolide contain a characteristic hydrogen-bonded 9,11-epoxy-14β-hydroxy system. They alkylate propanethiol in a process which involves opening of the epoxide function with neighboring hydroxyl assistance. The reaction may mimic the inhibition of tumor growth via selective alkylation of the thiol groups of key enzymes concerned with growth regulation.