When tested on parasite cultures at the concentration of 10 μM, some of these cruzain inhibitors exhibited a clear trypanocidal activity without toxicity towards host cells. Compounds 2 were also reported to be potent inhibitors of cruzain and rhodesain and SAR revealed that complications of ...
Utilidad de las escalas de riesgo en terapia dual Duración de la DAPT DAPT en situaciones especiales Recomendación del Consenso del Colegio Colombiano de Hemodinamia Conflicto de intereses BibliografíaShow full outline Tables (3) Tabla 1 Tabla 2 Tabla 3Revista...
All compounds except 3g were predicted to be CYP2D6 non-inhibitors, and all derivatives were predicted to be hepatotoxic and highly-bound to plasma binding protein. Compounds 3c, 3d, 3i and 3j show medium apparent MDCK permeability. The calculated BBB values of the analogues were within the ...
Enzyme phenotyping for the formation of ART-M (10β–hydroxyartemisinin) from artemisinin (ART; 1 µM) using human liver microsomes (HLM, 1 mg/mL) in the presence of (non)selective inhibitors of total P450 enzymes (1-ABT), CYP1A2 (α-naphthoflavone, NAPH), CYP2B6 (ticlopidine, TCL)...
The use of cytochrome P450 2D6-inhibiting drugs (CYP2D6 inhibitors) during tamoxifen treatment leads to a decrease in plasma concentration of endoxifen, th... VO Dezentje,NJC Van Blijderveen,H Gelderblom,... - 《Journal of Clinical Oncology Official Journal of the American Society of Clinical ...
Estrogen signaling is crucial for breast cancer initiation and progression. Endocrine-based therapies comprising estrogen receptor (ER) modulators and aromatase inhibitors remain the mainstay of treatment. This study aimed at investigating the antitumor
16 Nonselective NSAIDs inhibit both COX-1 and COX-2, whereas selective NSAIDs are exclusively COX-2 inhibitors.17 NSAIDs are commonly used as antipyretic, analgesic, and anti-inflammatory agents worldwide. NSAIDs are the first-line agents for mild-to-moderate musculoskeletal pain and ...
Inhibition of this isozyme by specific inhibitors or herbal drugs has been shown to be hepatoprotective [8-10]. Several reactive derivatives of drugs and oxidants are generated during the process of drug biotransformation. The reactive species generated can bind and/or react with cel...
Hence, COX-2 inhibitors have been tested for their anti-cancer therapeutic activity activity and showed potential as preventative agents [17,18]. In established tumours however, only overdose concentrations of paracetamol have demonstrated therapeutic potential [[19], [20], [21]]. Here we show ...
25,26 Sign in to download full-size image Even with the success of existing nucleos(t)ide HBV therapy, work has continued in an effort to identify novel inhibitors that may provide additional benefit relative to the existing agents, and several of the anti-HIV agents mentioned above have ...