Solid-phase synthesis of libraries of ethynylated aminosteroid derivatives as potential antileukemic agents
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- 作者：Amé ; lie Talbot ; René ; Maltais ; Lucie Carolle Kenmogne ; Jenny Roy ; Donald Poirier ; donald.poirier@crchul.ulaval.ca" class="auth_mail" title="E-mail the corresponding author
- 关键词：AA ; amino acid ; AcOH ; acetic acid ; 6-Cl-HOBt ; 6-chloro-1-hydroxybenzotriazole ; DCM ; dichloromethane ; DIPEA ; N ; N-diisopropylethylamine ; DMF ; N ; N-dimethylformamide ; Fmoc ; 9-fluorenylmethoxycarbonyl ; h ; hour ; HOBt ; 1-hydroxybenzotriazole hydrate ; HPLC ; high-performance liquid chromatography ; IR ; infrared spectroscopy ; MS ; mass spectrometry ; NMR ; nuclear magnetic resonance ; Pal ; pyridylalanine ; Phe ; phenylalanine ; Pro ; proline ; PS-DES ; polystyrene diethylsilyl resin ; PyBOP ; (benzotriazol-1-yloxy)tri
- 刊名：Steroids
- 出版年：2016
- 出版时间：March 2016
- 年：2016
- 卷：107
- 期：Complete
- 页码：55-64
- 全文大小：2764 K
文摘
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Libraries of hydroxy-acetylenic steroid derivatives were prepared.
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The usefulness of a diethylsilyl acetylenic linker for solid-phase synthesis was validated.
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A diethylsilyl acetylenic linker provided alcohols with better metabolic stability.
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Ethynylated steroid alcohols inhibit the cell proliferation of 2 leukemia cell lines.