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Relevant bibliographies by topics / Selenoorganic compounds, metabolic stability, CYP3A4 inhibition

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Journal articles

Academic literature on the topic 'Selenoorganic compounds, metabolic stability, CYP3A4 inhibition'

Author: Grafiati

Published: 24 April 2022

Last updated: 30 July 2025

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Journal articles on the topic "Selenoorganic compounds, metabolic stability, CYP3A4 inhibition"

1

Medvedíková, Martina, Václav Ranc, Ján Vančo, Zdeněk Trávníček, and Pavel Anzenbacher. "Highly Cytotoxic Copper(II) Mixed-Ligand Quinolinonato Complexes: Pharmacokinetic Properties and Interactions with Drug Metabolizing Cytochromes P450." Pharmaceutics 15, no. 4 (2023): 1314. http://dx.doi.org/10.3390/pharmaceutics15041314.

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The effects of two anticancer active copper(II) mixed-ligand complexes of the type [Cu(qui)(mphen)]Y·H2O, where Hqui = 2-phenyl-3-hydroxy- 1H-quinolin-4-one, mphen = bathophenanthroline, and Y = NO3 (complex 1) or BF4 (complex 2) on the activities of different isoenzymes of cytochrome P450 (CYP) have been evaluated. The screening revealed significant inhibitory effects of the complexes on CYP3A4/5 (IC50 values were 2.46 and 4.88 μM), CYP2C9 (IC50 values were 16.34 and 37.25 μM), and CYP2C19 (IC50 values were 61.21 and 77.07 μM). Further, the analysis of mechanisms of action uncovered a non-com

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2

Abram, Michał, Marcin Jakubiec, Anna Rapacz, et al. "The Search for New Anticonvulsants in a Group of (2,5-Dioxopyrrolidin-1-yl)(phenyl)Acetamides with Hybrid Structure—Synthesis and In Vivo/In Vitro Studies." International Journal of Molecular Sciences 21, no. 22 (2020): 8780. http://dx.doi.org/10.3390/ijms21228780.

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Epilepsy belongs to the most common and debilitating neurological disorders with multifactorial pathophysiology and a high level of drug resistance. Therefore, with the aim of searching for new, more effective, and/or safer therapeutics, we discovered a focused series of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant properties. We applied an optimized coupling reaction yielding several hybrid compounds that showed broad-spectrum activity in widely accepted animal seizure models, namely, the maximal electroshock (MES) test and the psychomotor 6 Hz (32 mA) seizure

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3

Attwa, Mohamed W., Haitham AlRabiah, Gamal A. E. Mostafa, and Adnan A. Kadi. "Evaluation of Alectinib Metabolic Stability in HLMs Using Fast LC-MS/MS Method: In Silico ADME Profile, P450 Metabolic Lability, and Toxic Alerts Screening." Pharmaceutics 15, no. 10 (2023): 2449. http://dx.doi.org/10.3390/pharmaceutics15102449.

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Alectinib, also known as Alecensa®, is prescribed for the therapeutic treatment of individuals diagnosed with metastatic non-small cell lung cancer (NSCLC) who have a specific genetic mutation referred to as anaplastic lymphoma kinase (ALK) positivity. The Food and Drug Administration granted regular approval to alectinib, a drug developed by Hoffmann-La Roche, Inc. (Basel, Switzerland)/Genentech, Inc. (South San Francisco, CA, USA), on 6 November 2017. The screening of the metabolic stability and identification of hazardous alarms within the chemical structure of ALC was conducted using the S

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4

Le Moigne, Ronan, Paul Pearson, Veronique Lauriault, et al. "Preclinical and clinical pharmacology of EPI-7386, an androgen receptor N-terminal domain inhibitor for castration-resistant prostate cancer." Journal of Clinical Oncology 39, no. 6_suppl (2021): 119. http://dx.doi.org/10.1200/jco.2021.39.6_suppl.119.

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119 Background: EPI-7386 is the newest of the “anitens”, a new class of compounds designed to inhibit androgen receptor activity by binding to the N-terminal domain (NTD) of the AR. Through this novel method of AR inhibition, anitens can block AR transcription even in the presence of AR ligand-binding domain (LBD) resistance mechanisms including point mutations and splice variants. Compared to the first generation aniten, EPI-506, which showed poor pharmacokinetic properties in patients, EPI-7386 is metabolically stable in vitro and in vivo. A Phase 1 clinical trial of EPI-7386 in metastatic c

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5

Annang, Frederick, Guiomar Pérez-Moreno, Caridad Díaz, et al. "Preclinical evaluation of strasseriolides A–D, potent antiplasmodial macrolides isolated from Strasseria geniculata CF-247,251." Malaria Journal 20, no. 1 (2021). http://dx.doi.org/10.1186/s12936-021-03993-8.

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Abstract Background Malaria is a global health problem for which novel therapeutic compounds are needed. To this end, a recently published novel family of antiplasmodial macrolides, strasseriolides A–D, was herein subjected to in vivo efficacy studies and preclinical evaluation in order to identify the most promising candidate(s) for further development. Methods Preclinical evaluation of strasseriolides A–D was performed by MTT-based cytotoxicity assay in THLE-2 (CRL-2706) liver cells, cardiotoxicity screening using the FluxOR™ potassium assay in hERG expressed HEK cells, LC–MS-based analysis

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