With the objective to understand structural features responsible for the biological activity, novel nonelectrophilic biphenyl derivatives and peptide-biphenyl hybrids have been synthesized and evaluated as calpain I inhibitors. The preliminary results indicate that the presence of additional aromatic rings (besides the biphenyl system) makes these compounds potent calpain inhibitors with IC50 values in the nanomolar range.
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http://dx.doi.org/10.1016/j.bmcl.2004.03.071 | DOI Listing |
Molecules
December 2024
Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, Traversa La Crucca 3, I-07100 Sassari, Italy.
In this study, UV-induced ()-to-() geometrical isomerizations of the curcumin degradation product ()-dehydrozingerone, along with curcumin-inspired ()--methylated dehydrozingerone and their corresponding C-symmetric dimers, were investigated. All compounds produced corresponding () isomers in varying yields upon UV irradiation in deuterated solvents. The efficiency of these photoisomerizations depended on the solvent and wavelength used.
View Article and Find Full Text PDFJ Med Chem
January 2025
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China.
The development of dual prostaglandin E receptors 2/4 (EP2/EP4) antagonists represents an attractive strategy for cancer immunotherapy. Herein, a series of 4,7-dihydro-5-thieno[2,3-]pyran derivatives with potent EP2/EP4 dual antagonism were discovered by fine-tuned structural modifications. The biphenyl side chain was found to be the key pharmacophore for the transition from EP4 antagonism to EP2/EP4 dual antagonism.
View Article and Find Full Text PDFLangmuir
January 2025
Department of Chemistry, Faculty of Science, Ilam University, P.O. Box 69315516, Ilam, Iran.
Beilstein J Org Chem
December 2024
Institut de Physique et Chimie des Matériaux de Strasbourg (IPCMS), CNRS-Université de Strasbourg (UMR 7504), F-67034 Strasbourg, France.
The high potential of non-covalent arene-fluoroarene intermolecular interactions in the design of liquid crystals lies in their ability to strongly promote self-assembly, improve the order and stability of the supramolecular mesophases, and enable tuneability of the optical and electronic properties, which can potentially be exploited for advanced applications in display technologies, photonic devices, sensors, and organic electronics. We recently successfully reported the straightforward synthesis of several mesogens containing four lateral aliphatic chains and derived from the classical triphenylene core self-assembling in columnar mesophases based on this paradigm. These mesogenic compounds were simply obtained in good yields by the nucleophilic substitution (SFAr) of various types of commercially available fluoroarenes with the electrophilic organolithium derivatives 2,2'-dilithio-4,4',5,5'-tetraalkoxy-1,1'-biphenyl (2Li- ).
View Article and Find Full Text PDFBMC Plant Biol
December 2024
Beichuan Shennong Agriculture Technology Development Co., Ltd, Mianyang, 621000, China.
Background: Magnolia officinalis (M. officinalis) thrives in temperate, elevated regions, and its desiccated bark comprises medicinal monolignol. Both abiotic and biotic factors can influence the pharmacodynamic compounds of M.
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