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A Triple High Throughput Screening for Extracellular Vesicle Inducing Agents With Immunostimulatory Activity.
Front Pharmacol
April 2022
Moores Cancer Center, University of California San Diego, La Jolla, CA, United States.
Extracellular vesicles (EVs) play an important role in intercellular communication and regulation of cells, especially in the immune system where EVs can participate in antigen presentation and may have adjuvant effects. We aimed to identify small molecule compounds that can increase EV release and thereby enhance the immunogenicity of vaccines. We utilized a THP-1 reporter cell line engineered to release EV-associated tetraspanin (CD63)-Turbo-luciferase to quantitatively measure EVs released in culture supernatants as a readout of a high throughput screen (HTS) of 27,895 compounds.
View Article and Find Full Text PDFSynthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides.
Mini Rev Med Chem
October 2019
Chemistry Department, Faculty of Science, Qassim University, Buraydah, Saudi Arabia.
Background & Objective: New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.
Methods: The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.
Results: The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines.
Design, Synthesis of New Pyridine and Pyrimidine Sugar Compounds as Antagonists Targeting the ERα via Structure-Based Virtual Screening.
Mini Rev Med Chem
March 2019
Department of Zoology, Faculty of Science Al-Azhar University, Cairo, Egypt.
Background: New aryl substituted cyclohepta[b]pyridine and cyclohepta[d]pyrimidine derivatives were synthesized. The sugar hydrazones of the synthesized pyridine and pyrimidine compounds were also prepared.
Method: In addition, the 1,3,4-oxadiazolyl acyclic C-nucleoside analogs of the pyridine system were prepared.
Photochemical and Electrochemical Triggered Bis(hydrazone) Switch.
Chemistry
October 2017
Departamento de Química, Facultad de Ciencias NaturalesyExactas, Universidad del Valle, A.A, 25360, Cali, Colombia.
Article Synopsis
- The study discusses the creation of a double hydrazone compound that can switch forms (E/Z isomerization) when exposed to light, functioning like a molecular machine.
- The compound exists in a "two-arm" configuration, allowing each arm to adjust its structure under light, resulting in two different stable forms (1-E,Z and 1-Z,Z).
- This research highlights the potential of using double hydrazones as customizable photochemical switches, which could advance the development of molecular machines and light-controlled reactions.
Metal ion-binding properties of DNA duplexes containing thiopyrimidine base pairs.
Chem Commun (Camb)
May 2012
Department of Material and Life Chemistry, Faculty of Engineering, Kanagawa University, 3-27-1 Rokkakubashi, Kanagawa-ku, Yokohama 221-8686, Japan.
Thiopyrimidine pairs in DNA duplexes were unexpectedly largely stabilized by complexation with two equivalents of Ag(I) ions and their binding properties were evaluated. The metal ion-binding properties of the thiopyrimidine base pairs differed significantly from those of unpaired bases.
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