Synthesis and Biological Evaluation of 4′-Substituted Kaempfer-3-ols

被引：12

作者：

Kim, Sugyeom ^{[5
]}

Li, Yu ^{[5
]}

Lin, Lin ^{[5
]}

Sayasith, Peyton R. ^{[5
]}

Tarr, Ariel T. ^{[5
]}

Wright, Eric B. ^{[4
,6
]}

Yasmin, Sharia ^{[4
,7
,8
]}

Lannigan, Deborah A. ^{[1
,2
,3
,4
]}

O'Doherty, George A. ^{[5
]}

机构：

[1] Vanderbilt Univ, Med Ctr, Dept Pathol Microbiol & Immunol, Nashville, TN 37232 USA

[2] Vanderbilt Univ, Med Ctr, Dept Cell & Dev Biol, Nashville, TN 37232 USA

[3] Vanderbilt Univ, Med Ctr, Dept Biomed Engn, Nashville, TN 37232 USA

[4] Vanderbilt Univ, Nashville, TN 37232 USA

[5] Northeastern Univ, Dept Chem & Chem Biol, Boston, MA 02115 USA

[6] Vanderbilt Univ, Med Ctr, Biomed Engn, Nashville, TN 37232 USA

[7] Vanderbilt Univ, Med Ctr, Dept Pathol, Nashville, TN 37232 USA

[8] Vanderbilt Univ, Med Ctr, Dept Microbiol & Immunol, Nashville, TN 37232 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 85卷 / 06期

基金：

美国国家科学基金会; 美国国家卫生研究院;

关键词：

BREAST-CANCER CELLS; 5A-CARBASUGAR ANALOGS; KINASE RSK; SL0101; INHIBITOR; AFFINITY; PATHWAY; DISCOVERY; GALANGIN; POTENT;

D O I：

10.1021/acs.joc.9b03461

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of two series of five kaempfer-3-ols was described. The first set all have a C-3 hydroxyl group and the second has a carboxymethoxy ether at the C-3 position. Both series have variable substitution at the C-4' position (i.e., OH, CI, F, H, OMe). Both kaempferols and carboxymethoxy ethers were evaluated for their ability to inhibit ribosomal s6 kinase (RSK) activity and cancer cell proliferation.

引用

页码：4279 / 4288

页数：10

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