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Discovery of -(2-Acetamidobenzo[]thiazol-6-yl)-2-phenoxyacetamide Derivatives as Novel Potential BCR-ABL1 Inhibitors Through Structure-Based Virtual Screening.
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National Institute for Viral Disease Control and Prevention, Chinese Center for Disease Control and Prevention, WHO Collaborating Centre for Reference and Research on Influenza, Key Laboratory for Medical Virology and Viral Diseases, National Health Commission, National Key Laboratory of Intelligent Tracking and Forecasting for Infectious Disease, Beijing 102206, China.
BCR-ABL1 kinase is a critical driver of chronic myeloid leukemia (CML) pathophysiology. The approval of allosteric inhibitor asciminib brings new hope for overcoming drug resistance caused by mutations in the ATP-binding site. To expand the chemical diversity of BCR-ABL1 kinase inhibitors with positive anti-tumor effect with asciminib, structure-based virtual screening and molecular dynamics simulations were employed to discover novel scaffolds.
View Article and Find Full Text PDFThe bioactivity of atraric acid as an inducer of cellular senescence in prostate cancer cells is retained by lipophilic derivatives.
Naunyn Schmiedebergs Arch Pharmacol
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Institute of Human Genetics, Jena University Hospital, Am Klinikum 1, 07740, Jena, Germany.
Esters have been described as bioactive chemical compounds. However, the presence of an ester as a functional group is often associated with hydrolytic liability. Therefore, it is often unclear whether esters serve as pro-drugs and are rather converted into bioactive drugs in cells.
View Article and Find Full Text PDFMonitoring of Propiolamide-Mediated Molecular Crosstalk between Ferroptosis and Apoptosis by Raman Spectroscopy.
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State Key Laboratory of Supramolecular Structure and Materials, College of Chemistry, Jilin University, Changchun 130012, P. R. China.
Inducing programmed cell death is an efficient strategy for cancer treatments, and a deep understanding of the molecular mechanisms underlying cell death pathways is of significance for the rational design of anticancer drugs. Herein, propiolamide-mediated crosstalk between ferroptosis and apoptosis is investigated. In situ monitoring of reactive oxygen species (ROS) formation and the structural changes of propiolamide compounds is achieved by Raman spectroscopy.
View Article and Find Full Text PDFUncovering the potential mechanism and bioactive compounds of Salviae Miltiorrhizae Radix et Rhizoma in attenuating diabetic retinopathy.
Phytomedicine
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The MOE Key Laboratory for Standardization of Chinese Medicines, Shanghai Key Laboratory of Compound Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China. Electronic address:
Background: Diabetic retinopathy (DR) is a serious microangiopathy resulting from diabetes. Salviae Miltiorrhizae Radix et Rhizoma (Danshen) is commonly used to treat cardiovascular diseases in clinics in China. However, whether it can also be used for DR treatment, along with its primary active compounds and underlying mechanisms of action, remains unclear.
View Article and Find Full Text PDFHalogenase-Assisted Biocatalytic Derivatization of Aminothiazoles and Cephalosporin Antibiotics.
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School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, Georgia 30332, United States.
With a view toward the prominence of brominated intermediates in chemical synthesis, we describe here a biocatalytic scheme for the enzymatic bromination of 2-aminothiazoles using a marine macroalgal brominase in reaction conditions that are directly compatible with Suzuki-Miyaura cross-coupling reactions. Enzymatically delivered brominated thiazoles, without intermediary purification, are arylated in high yields. We demonstrate the applicability of the methodology described herein in derivatizing clinically administered cephalosporin antibiotics and prodrugs in an aqueous solvent and mild reaction conditions.
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