Structure-activity relationships of epolactaene analogs as DNA polymerases inhibitors.
Structure-activity relationships of epolactaene analogs as DNA polymerases inhibitors.
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DOI：
10.1016/j.bmc.2004.03.007
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发表时间：
2004-05
影响因子：
3.5
通讯作者：
Kouji Kuramochi;Y. Mizushina;Seigo Nagata;F. Sugawara;K. Sakaguchi;Susumu Kobayashi
中科院分区：
文献类型：
--
作者：
Kouji Kuramochi;Y. Mizushina;Seigo Nagata;F. Sugawara;K. Sakaguchi;Susumu Kobayashi
Epolactaene是人神经母细胞瘤细胞中的一种促神经突化合物，对DNA聚合酶α和β具有抑制活性。介绍了依泊内酯类似物的合成及其抑制活性。环核中的α，β-环氧-γ-内酰胺基团和侧链的长度对活性有很大影响。化合物5是所有合成化合物中最强的DNA聚合酶α和β抑制剂，IC 50值分别为13和78μM。具有改性核心部分的N-和O-烷基衍生物显示出中度抑制。
Epolactaene, a neuritogenic compound in human neuroblastoma cells, showed inhibitory activities against DNA polymerases α and β. The synthesis and inhibitory activities of epolactaene analogs are described. The α,β-epoxy-γ-lactam moiety in the core and the length of the side chain greatly influenced the activities. Compound 5 was the strongest inhibitor of DNA polymerase α and β of all synthesized compounds with IC50values of 13 and 78μM, respectively. N- and O-alkyl derivatives that had modified core moieties showed moderate inhibition.