The development of a convergent fragment coupling strategy for the enantioselective total syntheses of a group of rearranged spongian diterpenoids that harbor the cis-2,8-dioxabicyclo[3.3.0]octan-3-one unit is described. The key bond disconnection relies on a late-stage fragment coupling between a tertiary carbon radical and an electron-deficient alkene to unite two ring systems and form two new stereocenters, one of which is quaternary, in a stereoselective and efficient manner. This strategy is applied toward scalable 14-15 step syntheses of three rearranged spongian diterpenoids, cheloviolenes A and B, and dendrillolide C.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1021/acs.joc.7b02458 | DOI Listing |
The human heterogeneous nuclear ribonucleoprotein (hnRNP) A1 is a prototypical RNA-binding protein essential in regulating a wide range of post-transcriptional events in cells. As a multifunctional protein with a key role in RNA metabolism, deregulation of its functions has been linked to neurodegenerative diseases, tumour aggressiveness and chemoresistance, which has fuelled efforts to develop novel therapeutics that modulates its RNA binding activities. Here, using a combination of Molecular Dynamics (MD) simulations and graph neural network pockets predictions, we showed that hnRNPA1 N-terminal RNA binding domain (UP1) contains several cryptic pockets capable of binding small molecules.
View Article and Find Full Text PDFZygote
January 2025
Molecular Medicine Research Center, Research Institute of Basic Medical Sciences, Rafsanjan University of Medical Sciences, Rafsanjan, Iran.
Recently, the World Health Organization recommendation for abstinence time for semen analysis has been challenged in some studies and many of them have supported the advantages of a second short abstinence ejaculation. More evidence is needed to approve this for clinical use. This study aimed to compare the average routine abstinence time (2-7 days) with the short time (1-2 h) on sperm quality based on functional parameters in a population of oligo-astheno-teratozoospermia (OAT) men.
View Article and Find Full Text PDFBMB Rep
January 2025
Division of Endocrinology and Metabolism, Department of Internal Medicine, Korea University College of Medicine, Seoul 02841, Korea.
G protein-coupled receptor 40 (GPR40) is gaining recognition as a potential therapeutic target for several metabolic disturbances, such as hyperglycemia and excessive inflammation. GPR40 is expressed in various tissues, including the heart; however, its specific roles in cardiomyocytes remain unknown. The objective of the present study was to investigate whether treatment with AM1638, a GPR40-full agonist, reduces palmitate-mediated cell damage in H9c2 rat cardiomyocytes.
View Article and Find Full Text PDFNat Chem
January 2025
Department of Chemistry, Scripps Research, La Jolla, CA, USA.
Amino alcohols are vital in natural products, pharmaceuticals and agrochemicals, and as key building blocks for various applications. Traditional synthesis methods often rely on polar bond retrosynthetic analysis, requiring extensive protecting group manipulations that complicate direct access. Here we show a streamlined approach using a serine-derived chiral carboxylic acid in stereoselective electrocatalytic decarboxylative transformations, enabling efficient access to enantiopure amino alcohols.
View Article and Find Full Text PDFIntroduction: Ethiopia has made notable progress in reducing maternal and perinatal mortality, yet challenges remain in meeting the 2030 Sustainable Development Goals. Persistent issues such as low service utilization, coupled with poor quality, fragmented care, and ineffective referral systems hinder progress. The "Improve Primary Health Care Service Delivery (IPHCSD)" project, implemented by JSI and Amref Health Africa since April 2022, seeks to address these gaps through a Networks of Care (NoCs) approach.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!