A series of aryloxy alkyl/aryl alkyl imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani. All the 19 compounds exhibited 94-100% inhibition at 10microg/mL against promastigotes and 12 compounds exhibited high inhibition with an IC(50) in the range of 0.47-4.85microg/mL against amastigotes. Promising compounds were tested further in vivo. Among all, compounds 4 and 23 with 4-CF(3) aryloxy moiety exhibited medium in vivo inhibition of 58-60%, thus providing new structural lead for antileishmanials.
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http://dx.doi.org/10.1016/j.bmcl.2009.10.117 | DOI Listing |
Mol Med
December 2024
Department of Neurobiology and Anatomy, Key Laboratory of Neurobiology, Xuzhou Medical University, 209, Tongshan Road, Xuzhou, 221004, China.
Doublecortin (DCX) is a microtubule-associated protein known to be a key regulator of neuronal migration and differentiation during brain development. However, the role of DCX, particularly in regulating the survival and growth of glioma cells, remains unclear. In this study, we utilized CRISPR/Cas9 technology to knock down DCX in the human glioma cell line (U251).
View Article and Find Full Text PDFClinics (Sao Paulo)
December 2024
Department of Emergency, Zhejiang Jinhua Guangfu Tumor Hospital, Zhejiang, PR China.
Objective: Based on Toll Like Receptor 4 (TLR4)/Nuclear Factor-κB (NF-κB) Exploring the effects of Licochalcone A (LCA) on the proliferation, invasion, and drug resistance of glioma cells through signaling pathways.
Methods: Cultivate human glioma cell line U251 in vitro, induce drug-resistant cell line U251/TMZ with Temozolomide (TMZ), and validate the results. Different concentrations of licorice chalcone A were used to treat U251 cells and U251/TMZ cells, and were named as control group, low-dose group, medium-dose group, and high-dose group, respectively.
Stem Cell Res Ther
December 2024
Department of Pathology, Sun Yat-sen Memorial Hospital, Sun Yat-sen University, 33 Ying Feng Road, Guangzhou, 510120, China.
Background: Cancer stem cells (CSCs) have unique metabolic characteristics and are hypothesized to contribute significantly to the recurrence and drug resistance of glioblastoma multiforme (GBM). However, the reliance on mitochondrial metabolism and the underlying mechanism of glioblastoma stem cells (GSCs) remains to be elucidated.
Methods: To quantify differential mitochondrial protein expression between GSCs and differentiated cells, a mass spectrum screen was applied by the Stable Isotope Labeling with Amino Acids in Cell Culture (SILAC) technique.
Pharm Res
December 2024
Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641Yamazaki, Noda-Shi, Chiba, 278-8510, Japan.
Purpose: Drug photodegradation is a matter of great concern because it can result in potency loss and adverse side effects. This study examines the light-induced degradation of dacarbazine catalyzed by vitamin B and flavin adenine dinucleotide (FAD) under light-emitting diode (LED) or fluorescent light irradiation.
Methods: Dacarbazine was irradiated with LED (405 nm) or fluorescent light in the presence of various equivalents of vitamin B or FAD.
Org Biomol Chem
December 2024
Alexander Butlerov Institute of Chemistry, Kazan Federal University, 18 Kremlevskaya Str., 420008 Kazan, Russia.
Efficient catalytic systems for various organic transformations in green solvents, especially water, are in great demand. Catalytically active bis-NHC complexes of palladium(II) based on imidazole-4,5-dicarboxylic acid with different lipophilicities were obtained. The synthesis of imidazolium salts was complicated by the formation of side products of nucleophilic substitution by iodide ions in the Menshutkin reaction involving alkyl iodides, which was successfully resolved by using alkyl tosylates.
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