2-Indazoles are one class of the most important nitrogen-containing heterocyclic compounds. The 2-indazole motif is widely present in bioactive natural products and drug molecules that exhibit distinctive bioactivities. Therefore, much attention has been paid to access diverse 2-indazole derivatives. Among them, the late-stage functionalization of 2-indazoles C-H activation is recognized as an efficient approach for increasing the complexity and diversity of 2-indazole derivatives. In this review, we summarized recent achievements in the late-stage functionalization of 2-indazoles, including the C3-functionalization of 2-indazoles through transition metal-catalyzed C-H activation or a radical pathway, transition metal-catalyzed C2'-H functionalization of 2-indazoles and remote C-H functionalization at the benzene ring in 2-indazoles.
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http://dx.doi.org/10.1039/d2ob01463g | DOI Listing |
J Chem Inf Model
January 2025
School of Information and Artificial Intelligence, Anhui Provincial Engineering Research Center for Beidou Precision Agriculture Information, Key Laboratory of Agricultural Sensors for Ministry of Agriculture and Rural Affairs, Anhui Agricultural University, Hefei, Anhui 230036, China.
Antimicrobial peptides (AMPs) are small peptides that play an important role in disease defense. As the problem of pathogen resistance caused by the misuse of antibiotics intensifies, the identification of AMPs as alternatives to antibiotics has become a hot topic. Accurately identifying AMPs using computational methods has been a key issue in the field of bioinformatics in recent years.
View Article and Find Full Text PDFNicotine Tob Res
January 2025
Department of Population Health Sciences, University of Leicester, Leicester, UK.
Introduction: Varenicline is an α4β2 nicotinic acetylcholine receptor partial agonist with the highest therapeutic efficacy of any pharmacological smoking cessation aid and a 12-month cessation rate of 26%. Genetic variation may be associated with varenicline response, but to date no genome-wide association studies of varenicline response have been published.
Methods: In this study, we investigated the genetic contribution to varenicline effectiveness using two electronic health record-derived phenotypes.
J Diet Suppl
January 2025
Department of Biomedical and Biotechnological Sciences, University of Catania, Catania, Italy.
Background: Several epidemiological studies and intervention trials have demonstrated that grapes and blueberries, which are rich in flavanols, can lower the risk of cardiovascular disease. However, the mechanisms of action of these compounds remain unclear due to their low bioavailability.
Objective: This study aimed to characterize the sensory properties, blood flow velocity, and oxidative stress of a polyphenol rich grape and blueberry extract (PEGB) containing approximately 16% flavanols (11% monomers and 4% dimers).
Elife
January 2025
Department of Molecular and Cell Biology, Berkeley, United States.
Type II nuclear receptors (T2NRs) require heterodimerization with a common partner, the retinoid X receptor (RXR), to bind cognate DNA recognition sites in chromatin. Based on previous biochemical and overexpression studies, binding of T2NRs to chromatin is proposed to be regulated by competition for a limiting pool of the core RXR subunit. However, this mechanism has not yet been tested for endogenous proteins in live cells.
View Article and Find Full Text PDFJ Cancer Res Ther
December 2024
Department of Oncology, Shandong Provincial Hospital Affiliated to Shandong First Medical University, P.R. China.
Background: Cryoablation induces antitumor immune responses. Spatial transcriptomic landscape technology has been used to determine the micron-level panoramic transcriptomics of tissue slices in situ.
Methods: The effects of cryoablation on the immune microenvironment in non-small cell lung cancer (NSCLC) were explored by comparing the Whole Transcriptome Atlas (WTA) panel of immune cells before and after cryoablation using the spatial transcriptomic landscape.
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