Enhancing the Potential of Miniature-Scale DNA-Compatible Radical Reactions via an Electron Donor–Acceptor Complex and a Reversible Adsorption to Solid Support Strategy
idiosyncratic needs and the required low concentration (∼1 mM or less) of the library intermediate. Here, we report visible-light-promoted on-DNA radical coupling reactions via an electrondonor–acceptor (EDA) complex and a reversible adsorption to solid support (RASS) strategy. This protocol provides a unique solution to the challenges of increasing the reactivity of highly diluted DNA substrates and reducing
DNA 编码文库 (DEL) 技术是发现生物活性探针分子和药物先导物的有力工具。大多数情况下,DEL 技术的成功源于化学库的分子多样性。然而,DEL 的构建受到特殊需求和所需的低浓度(~1 mM 或更低)的库中间体的限制。在这里,我们报告了可见光促进的 DNA 自由基偶联反应,通过电子供体 - 受体 (EDA) 复合物和固体载体的可逆吸附 (RASS) 策略。该协议为提高高度稀释的 DNA 底物的反应性和减少光催化剂中重金属残留的挑战提供了独特的解决方案。获得了一系列具有良好到定量转化的 DNA 上吲哚砜和硒化物衍生物。
Synthesis and anti-HIV-1 activity of a series of 1-(alkoxymethyl)-5-alkyl-6-(arylselenenyl)uracils and -2-thiouracils
作者:Dae-Kee Kim、Young-Woo Kim、Jongsik Gam、Ganghyeok Kim、Jinsoo Lim、Namkyu Lee、Hun-Taek Kim、Key H. Kim
DOI:10.1002/jhet.5570330446
日期:1996.7
e followed by reaction with an appropriate diaryl diselenide afforded 6-arylselenenyl compounds 18-26 after removal of the tert-butyldimethylsilyl protecting group and 35-47. Compounds 48-54 were prepared from compounds 38-44 by oxidative hydrolysis of the thione function. Of these compounds, 50 inhibited HIV-1 replication in human T4 lymphoblastoid cells at a 50% effective concentration (EC50) of
The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active ingredients and processes of preparation thereof. ##STR1## wherein R.sup.1 is ethyl or isopropyl; R.sup.2 is (3,5 dimethylphenyl)selenenyl; R.sup.3 is phenyl or methyl; X is oxygen; and Y is oxygen.
three-component reaction of alkynylaryl ketones bearing an ortho-methoxy group, element selenium, and arylboronic acid, providing a facile route to selenofunctionalized chromone products has been developed. This protocol features high efficiency and high regioselectivity, and the use of selenium powder as the selenium source. Mechanistic experiments indicated that the combined oxidative effect of (bis(tri