ANALOGS OF S-ADENOSYLHOMOCYSTEINE AS POTENTIAL INHIBITORS OF BIOLOGICAL TRANSMETHYLATION - SYNTHESIS OF ANALOGS WITH MODIFICATIONS AT 5'-THIOETHER LINKAGE
ANALOGS OF S-ADENOSYLHOMOCYSTEINE AS POTENTIAL INHIBITORS OF BIOLOGICAL TRANSMETHYLATION - SYNTHESIS OF ANALOGS WITH MODIFICATIONS AT 5'-THIOETHER LINKAGE
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DOI：
10.1021/jm00227a021
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发表时间：
1976-01-01
影响因子：
7.3
通讯作者：
COWARD, JK
中科院分区：
文献类型：
--
作者：
CHANG, CD;COWARD, JK
研究了5“-硫醚键被O或N等排体取代的S-腺苷高半胱氨酸类似物的合成。这些化合物被设计成抵抗5“-取代基的酶催化水解裂解。通过适当封闭的腺苷衍生物的烷基化或酰化制备了一种胺类似物和2种酰胺类似物。这些新的类似物被评价为儿茶酚O-甲基转移酶和tRNA甲基化酶的抑制剂，并且具有差的抑制活性。
The synthesis of S-adenosylhomocysteine analogues, in which the 5''-thioether linkage is replaced by an O or N isostere, was investigated. These compounds were designed to be resistant to enzyme-catalyzed hydrolytic cleavage of the 5''-substituent. One amine analogue and 2 amide analogues were prepared via alkylation or acylation of appropriately blocked adenosine derivatives. These new analogues were evaluated as inhibitors of catechol O-methyltransferase and tRNA methylases and have poor inhibitory activity.