- Synthesis, biophysical characterization, and anti-HIV-1 fusion activity of DNA helix-based inhibitors with a p-benzyloxyphenyl substituent at the 5′-nucleobase site
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DNA helix-based HIV-1 fusion inhibitors have been discovered as potent drug candidates. Introduction of hydrophobic groups to a nucleobase provides an opportunity to design inhibitors with novel structures and mechanisms of action. In this work, two novel nucleoside analogues (1 and 2) were synthesized and incorporated into four DNA duplex- and quadruplex-based inhibitors. All the molecules showed anti-HIV-1 fusion activity. The effect of the p-benzyloxyphenyl group and the attached linker on the helix formation and thermal stability were fully compared and discussed. Surface plasmon resonance analysis further indicated that inhibitors with the same DNA helix may still have variable reaction targets, mainly attributed to the different hydrophobic modifications.
- Tang, Yongjia,Han, Zeye,Guo, Jiamei,Tian, Yangli,Liu, Keliang,Xu, Liang
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- A ratiometric electrochemical sensor for selectively monitoring monoamine oxidase A in the live brain
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Herein, an electrochemical method for selectively sensing and accurately quantifying monoamine oxidase A (MAO-A) in the cortex and thalamus of a live mouse brain was reported. Using this tool, it was found that MAO-A increased Ca2+entry into neuronsviathe TPRM2 channel in the live mouse brain of an AD model.
- Zhang, Chuanping,Tang, Chenxiao,Mei, Yuxiao,Zhang, Limin,Zhu, Anwei,Tian, Yang
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supporting information
p. 6487 - 6490
(2021/07/07)
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- BTK Inhibitors and uses thereof
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The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
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- Rapid access to chroman-3-ones through gold-catalyzed oxidation of propargyl aryl ethers
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The two-step: Chroman-3-ones are important intermediates for organic synthesis and medicinal chemistry. However, their syntheses require multiple steps and are not efficient. By using gold-catalyzed alkyne oxidation, this versatile heterocycle can be prepared in only two steps from readily available phenols and with mostly high efficiencies (see scheme).
- Wang, Yanzhao,Ji, Kegong,Lan, Sylvester,Zhang, Liming
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supporting information; experimental part
p. 1915 - 1918
(2012/03/26)
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- A hierarchy of aryloxide deprotection by boron tribromide
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Aryl propargyl ethers and esters are cleaved selectively in the presence of aryl methyl ethers and esters by boron tribromide in dichloromethane. Under the same conditions, allyl ethers undergo very rapid Claisen rearrangement, and benzyl ethers are also cleaved more rapidly than propargyl. A mechanism involving intramolecular delivery of bromide to the propargyl terminus is proposed.
- Punna, Sreenivas,Meunier, Stephane,Finn
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p. 2777 - 2779
(2007/10/03)
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