Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
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DOI：
10.1016/j.bmcl.2009.02.125
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发表时间：
2009-04-15
影响因子：
2.7
通讯作者：
Lindsley CW
中科院分区：
文献类型：
--
作者：
Lavieri R;Scott SA;Lewis JA;Selvy PE;Armstrong MD;Alex Brown H;Lindsley CW
This Letter describes the synthesis and structure–activity relationships (SAR) of isoform-selective PLD inhibitors. By virtue of the installation of a 1,3,8-triazaspiro[4,5]decan-4-one privileged structure, PLD inhibitors with nanomolar potency and an unprecedented 40-fold selectivity for PLD2 over PLD1 were developed. Interestingly, SAR for this diverged from our earlier efforts, and dual PLD1/2 inhibitors were also discovered within this series.
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影响因子：
14.8
作者：
Scott, Sarah A.;Selvy, Paige E.;Buck, Jason R.;Cho, Hyekyung P.;Criswell, Tracy L.;Thomas, Ashley L.;Armstrong, Michelle D.;Arteaga, Carlos L.;Lindsley, Craig W.;Brown, H. Alex
通讯作者：
Brown, H. Alex
影响因子：
2.7
作者：
Monovich, Lauren;Mugrage, Benjamin;Steed, Paul
通讯作者：
Steed, Paul
影响因子：
4.7
作者：
Min, DS;Kwon, TK;Jo, YH
通讯作者：
Jo, YH
DOI：
10.1006/bbrc.2000.3719
发表时间：
2000-11-11
影响因子：
3.1
作者：
Zhao, YT;Ehara, H;Nozawa, Y
通讯作者：
Nozawa, Y
影响因子：
2.7
作者：
Lindsley, CW;Zhao, ZJ;Duggan, ME
通讯作者：
Duggan, ME