Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators.

Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators.
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作为蛋白激酶 C 调节剂的 (2S,5R,6R)- 和 (2S,5R,6S)-6-羟基-8-(1-癸炔基)-苯并内酰胺-V8 的合成和建模研究。

DOI:
10.1021/ol026013u
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发表时间:
2002
期刊:
影响因子:
5.2
通讯作者:
Kozikowski,AlanP
Kozikowski,AlanP
中科院分区:
化学1区
文献类型:
--
作者:
Wei,Zhi-Liang;Sakamuri,Sukumar;Petukhov,PavelA;George,Clifford;Lewin,NancyE;Blumberg,PeterM;Kozikowski,AlanP

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Both (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy-8-(1-decynyl)benzolactam-V8 were designed and synthesized as PKC modulators. Biological assays reveal the (6R)-ligand to be 20-fold more potent than its (6S)-counterpart in binding to PKCα.