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MK-8776 and Olaparib Combination Acts Synergistically in Hepatocellular Carcinoma Cells, Demonstrating Lack of Adverse Effects on Liver Tissues in Ovarian Cancer PDX Model.
Int J Mol Sci
January 2025
Department of Medical Biophysics, Institute of Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, 90-236 Lodz, Poland.
Hepatocellular carcinoma (HCC) cells critically depend on PARP1 and CHK1 activation for survival. Combining the PARP inhibitor (PARPi) olaparib with a CHK1 inhibitor (MK-8776, CHK1i) produced a synergistic effect, reducing cell viability and inducing marked oxidative stress and DNA damage, particularly in the HepG2 cells. This dual treatment significantly increased apoptosis markers, including γH2AX and caspase-3/7 activity.
View Article and Find Full Text PDFD-Histidine modulated chiral metal-organic frameworks for discriminating 3,4-Dihydroxyphenylalanine enantiomers based on a chemiluminescence quenching mode.
Anal Chim Acta
February 2025
Key Laboratory of Luminescence Analysis and Molecular Sensing (Ministry of Education), College of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, China. Electronic address:
Background: Drug enantiomers often display distinguishable or even opposite pharmacological and toxicologic activities. Therefore it is of great necessity to discriminate enantiomers for guaranteeing safetyness and effectiveness of chiral drugs. Facile chiral discrimination has long been a noticeable challenge because of the minimal differences in physicochemical properties of enantiomers.
View Article and Find Full Text PDFCurrent strategies in design and synthesis of antifungals hybrid and chimeric diazine derivatives.
Bioorg Med Chem
January 2025
Alexandru Ioan Cuza University of Iasi, Faculty of Chemistry, Bd. Carol 11, 700506 Iasi, Romania. Electronic address:
In the last decades fungal infections became a major threat to human health having an unacceptably occurrence, a high rate of mortality and the number of patients at risk for these infections continue to increase every year. An effective, modern and very useful strategy in antifungal therapy is represented by the use of chimeric and hybrid drugs, most of them being with azaheterocycle skeleton. In this review, we present an overview from the last five years of the most representative achievements in the field of chimeric and hybrid diazine derivatives with antifungal properties.
View Article and Find Full Text PDFBlock Electrochemiluminescence of Luminol through O-Etherification and Its Application in Sensing of β-Glucosidase.
Anal Chem
January 2025
School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510632, China.
Luminol is a well-known electrochemiluminescence (ECL) fluorophore that is applied in various sensing fields as an ECL reporter. Regulating the signal off/on transition of an ECL fluorophore offers great opportunities for sensors' design; however, such attempts on luminol are extremely scarce as it was regarded to lack promising modification sites. In this study, we developed four luminol derivatives with modification at the amine site and the enol site and systematically explored possible caging strategies to regulate ECL emission.
View Article and Find Full Text PDFDiscovery of 2-(6-{[(1R,2R)-2-hydroxycyclohexyl]amino}-4,5-dimethylpyridazin-3-yl)-5-(trifluoromethyl)phenol (ASP0965): A potent, orally active and brain-penetrable NLRP3 inflammasome inhibitor with a novel scaffold for the treatment of α-synucleinopathy.
Bioorg Med Chem
February 2025
Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.
NLRP3 inflammasome inhibitor is a highly attractive drug target for the treatment of various inflammatory diseases. Here, we report the discovery of pyridazine derivatives as a new class of scaffold for NLRP3 inflammasome inhibitors. We optimized HTS hit 2a to improve both in vitro IL-1β inhibitory activity and the mean photo effect (MPE) value in the in vitro 3T3 neutral red uptake (NRU) phototoxicity test.
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