Results 21 to 30 of about 425,696 (264)

Synthesis, Molecular Structure, Metabolic Stability and QSAR Studies of a Novel Series of Anticancer N-Acylbenzenesulfonamides

open access: yesMolecules, 2015
A series of novel N-acyl-4-chloro-5-methyl-2-(R1-methylthio)benzenesulfonamides 18–47 have been synthesized by the reaction of N-[4-chloro-5-methyl-2-(R1-methylthio) benzenesulfonyl]cyanamide potassium salts with appropriate carboxylic acids.
Beata Żołnowska   +7 more
doaj   +1 more source

A Fast LC-MS/MS Methodology for Estimating Savolitinib in Human Liver Microsomes: Assessment of Metabolic Stability Using In Vitro Metabolic Incubation and In Silico Software Analysis

open access: yesSeparations, 2023
Savolitinib (Orpathys®), was developed by (HUTCHMED (Shanghai, China) and, AstraZeneca (Gaithersburg, Maryland, USA), is an inhibitor of the c-Met receptor tyrosine kinase that is orally bioavailable.
Mohamed W. Attwa   +3 more
doaj   +1 more source

A Rapid and Sensitive UPLC-MS/MS Method for Quantifying Capmatinib in Human Liver Microsomes: Evaluation of Metabolic Stability by In Silico and In Vitro Analysis

open access: yesSeparations, 2023
Capmatinib (CMB) is an orally bioavailable mesenchymal–epithelial transition (MET) inhibitor approved by the US-FDA to treat metastatic non-small cell lung cancer (NSCLC) patients, with MET exon 14 skipping mutation.
Mohamed W. Attwa   +3 more
doaj   +1 more source

Stabilizing selection and metabolism [PDF]

open access: yesHeredity, 1988
This paper attempts to provide a biochemical explanation for selection against extreme phenotypes. From current ideas on the analysis of metabolic control, it is argued that, on average, most mutations will reduce flux through metabolic pathways and change substrate pool concentrations in an arbitrary direction.
openaire   +2 more sources

A highly sensitive LC-MS/MS method to determine novel Bruton's tyrosine kinase inhibitor spebrutinib: application to metabolic stability evaluation [PDF]

open access: yesRoyal Society Open Science, 2019
Spebrutinib (SBT) is a Bruton's tyrosine kinase inhibitor. SBT is currently in phase II and phase I clinical trials for the management of rheumatoid arthritis and chronic lymphocytic leukaemia, respectively.
Ali S. Abdelhameed   +3 more
doaj   +1 more source

Development of a Fast and Sensitive UPLC–MS/MS Analytical Methodology for Fenebrutinib Estimation in Human Liver Microsomes: In Vitro and In Silico Metabolic Stability Evaluation

open access: yesSeparations, 2023
Fenebrutinib (GDC-0853; FNB) is an oral small molecule that was developed by Roche Pharmaceuticals to slow multiple sclerosis progression. FNB is a reversible bruton tyrosine kinase (BTK) inhibitor, which showed the maximum potency of BTK inhibitors in ...
Mohamed W. Attwa   +4 more
doaj   +1 more source

Connecting Hsp70, sphingolipid metabolism and lysosomal stability [PDF]

open access: yesCell Cycle, 2010
Heat shock protein 70 (Hsp70) is an evolutionary highly conserved molecular chaperone. Upon cancer-associated translocation to the lysosomal compartment, it promotes cell survival by inhibiting lysosomal membrane permeabilization, a hallmark of stress-induced death. We have recently shown that Hsp70 stabilizes lysosomes by binding to the endo-lysosomal
Nikolaj H T, Petersen   +3 more
openaire   +2 more sources

Pharmaceutical and Safety Profile Evaluation of Novel Selenocompounds with Noteworthy Anticancer Activity

open access: yesPharmaceutics, 2022
Prior studies have reported the potent and selective cytotoxic, pro-apoptotic, and chemopreventive activities of a cyclic selenoanhydride and of a series of selenoesters.
Małgorzata Anna Marć   +6 more
doaj   +1 more source

Epigenetic and Genetic Integrity, Metabolic Stability, and Field Performance of Cryopreserved Plants

open access: yesPlants, 2021
Cryopreservation is considered an ideal strategy for the long-term preservation of plant genetic resources. Significant progress was achieved over the past several decades, resulting in the successful cryopreservation of the genetic resources of diverse ...
Min-Rui Wang   +7 more
doaj   +1 more source

Novel 5-Substituted 2-(Aylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl)benzenesulfonamides: Synthesis, Molecular Structure, Anticancer Activity, Apoptosis-Inducing Activity and Metabolic Stability

open access: yesMolecules, 2016
A series of novel 5-substituted 2-(arylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl) benzenesulfonamide derivatives 27–60 have been synthesized by the reaction of aminoguanidines with an appropriate phenylglyoxal hydrate in glacial acetic acid.
Beata Żołnowska   +9 more
doaj   +1 more source

Home - About - Disclaimer - Privacy