De novo synthesis and biological evaluation of C6″-substituted C4″-amide analogues of SL0101.
De novo synthesis and biological evaluation of C6″-substituted C4″-amide analogues of SL0101.
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DOI：
10.1021/ol503012k
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发表时间：
2014-11-21
期刊：
影响因子：
5.2
通讯作者：
O'Doherty, George A.
中科院分区：
文献类型：
--
作者：
Mrozowski, Roman M.;Sandusky, Zachary M.;Vemula, Rajender;Wu, Bulan;Zhang, Qi;Lannigan, Deborah A.;O'Doherty, George A.
In an effort to improve upon the in vivo half-life of the known ribosomal s6 kinase (RSK) inhibitor SL0101, C4″-amide/C6″-alkyl substituted analogues of SL0101 were synthesized and evaluated in cell-based assays. The analogues were prepared using a de novo asymmetric synthetic approach, which featured Pd-π-allylic catalyzed glycosylation for the introduction of a C4″-azido group. Surprisingly replacement of the C4″-acetate with a C4″-amide resulted in analogues that were no longer specific for RSK in cell-based assays.
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影响因子：
16
作者：
Eisinger-Mathason, T. S. Karin;Andrade, Josefa;Groehler, Angela L.;Clark, David E.;Muratore-Schroeder, Tara L.;Pasic, Lejla;Smith, Jeffrey A.;Shabanowitz, Jeffrey;Hunt, Donald F.;Macara, Ian G.;Lannigan, Deborah A.
通讯作者：
Lannigan, Deborah A.
DOI：
10.1073/pnas.82.3.742
发表时间：
1985-01-01
影响因子：
11.1
作者：
ERIKSON, E;MALLER, JL
通讯作者：
MALLER, JL
影响因子：
2.7
作者：
Eisinger-Mathason, T. S. Karin;Andrade, Josefa;Lannigan, Deborah A.
通讯作者：
Lannigan, Deborah A.
影响因子：
3.5
作者：
Smith, Jeffrey A.;Maloney, David J.;Lannigan, Deborah A.
通讯作者：
Lannigan, Deborah A.
影响因子：
11.4
作者：
Wang, XM;Li, W;Proud, CG
通讯作者：
Proud, CG