Monocarbonyl curcuminoids as antituberculosis agents with their moderate in‐vitro metabolic stability on human liver microsomes
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.22754
Abstract: Tuberculosis, an airborne infectious disease, results in a high morbidity and mortality rate. The continuous emergence of TB resistance strains including MDR (multidrug‐resistant tuberculosis), XDR (extensive drug‐resistant tuberculosis), and especially TDR (totally drug‐resistant tuberculosis) is… read more here.
Keywords: vitro metabolic; metabolic stability; monocarbonyl curcuminoids; tuberculosis ... See more keywords
Application of MetMax™ pooled donor human hepatocytes in a higher throughput assay for human hepatic metabolic stability screening
Sign Up to like & getrecommendations! Published in 2018 at "Drug Metabolism and Pharmacokinetics"
DOI: 10.1016/j.dmpk.2017.11.208
Abstract: • Both MetMaxTM and Intact Human Hepatocytes yielded data comparable to clinical systemic clearance One interesting finding was that MetMaxTM hepatocytes were superior to pooled cryopreserved human hepatocytes in the evaluation of afatinib, a drug… read more here.
Keywords: stability screening; metabolic stability; pooled donor; drug ... See more keywords
Tetrazolylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.10.021
Abstract: A series of derivatives of 1-(4-octylphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one (3) and 1-(4-octylphenoxy)-3-(1H-tetrazol-1-yl)propan-2-one (4) was synthesized and tested for fatty acid amide hydrolase (FAAH) inhibitory potency and phase I metabolic stability. Introduction of certain substituents like 4-chlorophenyl, 4-methoxycarbonylphenyl and… read more here.
Keywords: acid amide; metabolic stability; fatty acid; amide hydrolase ... See more keywords
Minor chemical modifications of the aminosteroid derivative RM-581 lead to major impact on its anticancer activity, metabolic stability and aqueous solubility.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111990
Abstract: The aminosteroid (AM) RM-581 is built around a mestranol backbone and has recently emerged as this family's lead candidate, showing in vitro and in vivo potency over different types of cancer, including high fatality pancreatic cancer. To… read more here.
Keywords: cancer; activity; metabolic stability; anticancer activity ... See more keywords
Synthesis of 17β-hydroxysteroid dehydrogenase type 10 steroidal inhibitors: Selectivity, metabolic stability and enhanced potency.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112909
Abstract: 17beta-Hydroxysteroid dehydrogenase type 10 (17β-HSD10) is the only mitochondrial member of 17β-HSD family. This enzyme can oxidize estradiol (E2) into estrone (E1), thus reducing concentration of this neuroprotective steroid. Since 17β-HSD10 possesses properties that suggest… read more here.
Keywords: steroidal; hydroxysteroid dehydrogenase; metabolic stability; dehydrogenase type ... See more keywords
Validated LC-MS/MS assay for quantification of the newly approved tyrosine kinase inhibitor, dacomitinib, and application to investigating its metabolic stability
Sign Up to like & getrecommendations! Published in 2019 at "PLoS ONE"
DOI: 10.1371/journal.pone.0214598
Abstract: Dacomitinib (DMB) is a second-generation irreversible tyrosine kinase inhibitor (TKI) that is claimed to overcome the disadvantages of the resistance reported for first-line epidermal growth factor receptor (EGFR) TKIs. Towards the end of 2018, the… read more here.
Keywords: validated assay; metabolic stability; kinase inhibitor; quantification ... See more keywords
Metabolic Stability Assessment of Larotrectinib Using Liquid Chromatography Tandem Mass Spectrometry
Sign Up to like & getrecommendations! Published in 2020 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s235934
Abstract: Introduction Larotrectinib (VITRAKVI) is an orally potent tropomyosin receptor kinase (Trk) inhibitor that acts by competitive inhibition of all corresponding receptor kinases. It demonstrated a marked response rate (75%) and robust anticancer activity in Trk… read more here.
Keywords: metabolic stability; larotrectinib using; assessment larotrectinib; stability ... See more keywords
Metabolism of Peptide Drugs and Strategies to Improve their Metabolic Stability.
Sign Up to like & getrecommendations! Published in 2018 at "Current drug metabolism"
DOI: 10.2174/1389200219666180628171531
Abstract: BACKGROUND Despite the therapeutic use of peptides is limited because of their metabolism in vivo, there are no systematic reviews explaining degradation of peptides by peptidases. This review summarizes peptidases present in the tissues and… read more here.
Keywords: improve metabolic; metabolic stability; metabolism; peptide drugs ... See more keywords
Identification of Selective CYP3A7 and CYP3A4 Substrates and Inhibitors Using a High-Throughput Screening Platform
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.899536
Abstract: Cytochrome P450 (CYP) 3A7 is one of the major xenobiotic metabolizing enzymes in human embryonic, fetal, and newborn liver. CYP3A7 expression has also been observed in a subset of the adult population, including pregnant women,… read more here.
Keywords: cyp3a7; identification selective; p450 glo; metabolic stability ... See more keywords
Metabolic stability and metabolite profiling of emerging synthetic cathinones
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2023.1145140
Abstract: Synthetic cathinones constitute the second largest groups of new psychoactive substances (NPS), which are especially popular among adolescents and young adults. Due to their potential toxicity, the recreational use of these NPS constitute a serious… read more here.
Keywords: metabolite profiling; profiling emerging; stability metabolite; metabolic stability ... See more keywords
2-Oxoester Phospholipase A2 Inhibitors with Enhanced Metabolic Stability
Sign Up to like & getrecommendations! Published in 2020 at "Biomolecules"
DOI: 10.3390/biom10030491
Abstract: 2-Oxoesters constitute an important class of potent and selective inhibitors of human cytosolic phospholipase A2 (GIVA cPLA2) combining an aromatic scaffold or a long aliphatic chain with a short aliphatic chain containing a free carboxylic… read more here.
Keywords: oxoester; metabolic stability; phospholipase; stability ... See more keywords