Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related death throughout the world. Due to the shortcomings of traditional chemotherapy, targeted therapies have come into prominence for the management of NSCLC. In particular, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) therapy has emerged as a first-line therapy for NSCLC patients with EGFR-activating mutations. In this context, new indenopyrazoles, which were prepared by an efficient microwave-assisted method, were subjected to in silico and in vitro assays to evaluate their potency as EGFR TK-targeted anti-NSCLC agents. Compound 4 was the most promising antitumor agent towards A549 human lung adenocarcinoma cells, with an IC50 value of 6.13 µM compared to erlotinib (IC50 = 19.67 µM). Based on its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), it can be concluded that compound 4 exerts selective antitumor action. This compound also inhibited EGFR TK with an IC50 value of 17.58 µM compared to erlotinib (IC50 = 0.04 µM) and induced apoptosis (56.30%). Taking into account in silico and in vitro data, compound 4 stands out as a potential EGFR TKI for the treatment of NSCLC. 相似文献
Ionics - A new electrode composed of sepiolite clay (SC) carbon paste (CP) was developed and used for the adsorptive stripping differential pulse voltammetric quantification of ascorbic acid (AA).... 相似文献
An electrochemical biosensor for detection of fructose in food samples was developed by immobilization of fructose dehydrogenase (FDH) on cysteamine and poly(amidoamine) dendrimers (PAMAM)-modified gold electrode surface. Electrochemical analysis was carried out by using hexacyanoferrate (HCF) as a mediator and the response time was 35 s at +300 mV vs. Ag/AgCl. Moreover, some parameters such as pH, enzyme loading and type of PAMAM (Generations 2, 3 and 4) were investigated. Then, the FDH biosensor was calibrated for fructose in the concentration range of 0.25–5.0 mM. To evaluate its utility, the FDH biosensor was applied for fructose analysis in real samples. Finally, obtained data were compared with those measured with HPLC as a reference method. 相似文献
The electron paramagnetic resonance (EPR) spectra of Cu2+-doped RbH2 PO4 at elevated temperatures indicate a phase transition at 358 K. The EPR-silent state at this temperature is attributed to a so-called polymeric phase transition. After the transition when the temperature is lowered to 293 K, the EPR signal does not appear; therefore, the transition is irreversible. This result seems to be in agreement with the other observations. The EPR spectra for the sample indicate the presence of two sites for Cu2+, and the values of EPR parameters are in accord with the literature on Cu2+-doped single crystals. Any other phase transitions could not to be observed at low temperatures down to 113 K. 相似文献
Conventional cancer treatments such as chemotherapy, radiotherapy, or combination of these two result in side effects, which lower the quality of life of the patients. To overcome problems with these methods, altering the drug properties by conjugating them to carrier polymers has emerged. Such polymeric carriers also hold the potential to make tumor cells more sensitive to radiation therapy. Herein, poly(p‐phenylene) (PPP) polymer with poly(ethylene glycol) (PEG) chains and primary amino groups (PPP‐NH2‐g‐PEG) is synthesized and conjugated with anticancer drug Doxorubicin (DOX). pH dependent drug release experiments are performed at pH 5.3 and pH 7.4, respectively. Cell viability studies on human cervix adenocarcinoma cells show that lower doses of DOX inhibit cell proliferation when conjugated with nontoxic doses of PPP‐NH2‐g‐PEG polymer. Additionally, PPP‐NH2‐g‐PEG/Cys/DOX bioconjugate significantly increases radiosensitive properties of DOX. It is possible to use lower doses of DOX when conjugated to PPP‐NH2‐g‐PEG in combination with radiotherapy.