The study of non-oxazole containing indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis and in vitro inhibitory values for IMPDH II are discussed.
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http://dx.doi.org/10.1016/j.bmcl.2006.01.089 | DOI Listing |
Molecules
January 2025
Institute of Chemistry and Chemical Technology, Faculty of Natural Sciences and Technology, Riga Technical University, P. Valdena Str. 3, LV-1048 Riga, Latvia.
A metal-free two-step synthetic approach for obtaining indole derivatives from aryl triazole fragment-containing compounds has been developed. In the first step, the Dimroth equilibrium, followed by nitrogen extrusion, Wolff rearrangement, and amine nucleophile addition, leads to the formation of -aryl ethene-1,1-diamines. In the second step, the latter intermediates are cyclized into the target 1-indoles in the presence of iodine.
View Article and Find Full Text PDFBMJ Open
January 2025
IRCCS Mondino Foundation, Pavia, Italy
Introduction: Children with septo-optic-pituitary dysplasia (SOD) may experience a range of visual impairments and hormonal dysfunctions beyond developmental delay/intellectual disability. The literature describes sleep fragmentation, circadian rhythm disruptions and reduced sleep efficiency. These manifestations are believed to be closely linked to both structural and functional abnormalities associated with SOD, potentially disrupting the natural circadian rhythm.
View Article and Find Full Text PDFJ Extracell Vesicles
January 2025
Shanghai Jiao Tong University Affiliated Sixth People's Hospital, School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai, China.
Extracellular vesicles (EVs) have shown great potential for treating various diseases. Translating EVs-based therapy from bench to bedside remains challenging due to inefficient delivery of EVs to the injured area and lack of techniques to visualize the entire targeting process. Here we developed a dopamine surface functionalization platform that facilitates easy and simultaneous conjugation of targeting peptide and multi-mode imaging probes to the surface of EVs.
View Article and Find Full Text PDFPharmaceuticals (Basel)
November 2024
Departamento de Mantenimiento Industrial y Nanotecnología, Universidad Tecnológica de Ciudad Juárez, Maestría en Ingeniería Industrial Sustentable, Av. Universidad Tecnológica No. 3051, Col. Lote Bravo II, Ciudad Juárez 32695, Chihuahua, Mexico.
Breast cancer is a disease with a high mortality rate worldwide; consequently, urgent achievements are required to design new greener drugs, leaving natural products and their derivatives as good options. A constant antineoplastic effect has been observed when the phytoproduct contains an indole fragment. Therefore, the objective of this work was to carry out a thoughtful computational study to perform an appropriate evaluation of four novel molecules of the class of the 3-indolylquinones as phytodrug candidates for antineoplastic activity: thymoquinone (TQ), 2,6-dimethoxy-1,4-benzoquinone (DMQ), 2,3-dimethoxy-5-methyl-1,4-benzoquinone (DMMQ), and 2,5-dihydroxy-1,4-benzoquinone (DHQ).
View Article and Find Full Text PDFBiomolecules
December 2024
Department of Chemistry & Biochemistry, Texas Christian University, Fort Worth, TX 76129, USA.
The functionalization of protein sidechains with highly water-soluble chlorotriazines (or derivatives thereof) using nucleophilic aromatic substitution reactions has been commonly employed to install various functional groups, including poly(ethylene glycol) tags or fluorogenic labels. Here, a poorly soluble dichlorotriazine with an appended indole is shown to react with a construct containing the disordered domain of BRCA1. Subsequently, this construct can undergo proteolytic cleavage to remove the SUMO-tag: the -terminal poly(His) tag is still effective for purification.
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