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871.
Prof. Michael Murray Dr. Ariane Roseblade Dr. Yongjuan Chen Kirsi Bourget Dr. Tristan Rawling 《ChemMedChem》2020,15(2):247-255
Targeting the tumor cell mitochondrion could produce novel anticancer agents. We designed an aryl−urea fatty acid ( 1 g ; 16({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)hexadecanoic acid) that disrupted the mitochondrion and decreased MDA-MB-231 breast cancer cell viability. To optimize the aryl−ureas the present study evaluated mitochondrial targeting by 1 g analogues containing alkyl chains between 10–17 carbons. Using the dye JC-1, the C12−C17 analogues efficiently disrupted the mitochondrial membrane potential (IC50s 3.5±1.2 to 7.6±1.1 μM) and impaired ATP production; shorter analogues were less active. 7-Aminoactinomycin D/annexin V staining and flow cytometry showed that these agents activated the killing mechanisms of necrosis and apoptosis to varying extents (7-aminoactinomycin D/annexin V staining ratios 4.3–6.0). Indeed, 1 g and its C17 analogue preferentially activated necrosis and apoptosis, respectively (ratios 2.1 and 16). Taken together, alkyl chain length is a determinant of mitochondrial targeting by aryl−ureas and can be varied to develop analogues that activate apoptosis or necrosis in a regulated fashion. 相似文献
872.
The solvent-dependent polymorphism of the active pharmaceutical ingredient (API) carbamazepine is interpreted from calculations of the solid-state and API-solvent intermolecular interactions. These simulations suggested that apolar solute-solute interactions could be disrupted by apolar solvents. In contrast, the polar solute-solute interactions were found to be easily disrupted by polar and protic solvents. This is consistent with experimental observations that the crystallization of the metastable form II is more dominant in apolar solvents. The Mercury program remains the gold standard in terms of usability; however, further expansion into more complex simulation techniques could make this package of even greater use in pharmaceutical manufacturing workflows. 相似文献
873.
Ajit Sharma Doan Van Thuan Thanh-Dong Pham Mai Hung Thanh Tung Nguyen Thi Thanh Truc Dai-Viet N. Vo 《化学工程与技术》2020,43(4):752-761
FeO-doped TiO2 nanoparticle photocatalysts were immobilized onto the surface of fibrous activated carbon (ACF) via a sol-gel process. As an adsorbent and photocatalyst, FeO-TiO2 on immobilized ACFs (FeO-TiO2/ACF) greatly improved the photocatalysis rate of hydrogen production as compared with pure TiO2 and ACF-TiO2 under UV irradiation and visible light. The addition of ACFs surface significantly reduced the photogenerated pairs of electrons-hole recombination, thereby promoting the photocatalysis action of doped photo-metal oxides of FeO-TiO2. Co-doping of FeO onto the lattice of the TiO2 approach can improve the absorption activity of visible light through photo-metal oxide of TiO2 and further enhance hydrogen production under visible light. The photocatalytic fabrics (FeO-TiO2/ACF) were effortlessly split out from the experimental solution for re-utilization and exhibited high stability even after five complete regeneration cycles. 相似文献
874.
Radiochemistry - Leaching of uranium and REEs with oxalic acid from the Egyptian Abu-Tartur phosphate rock (PR) was studied. The effect exerted on the leaching process by oxalic acid concentration,... 相似文献
875.
Burdin D. A. Savel’ev D. V. Ekonomov N. A. Chashin D. V. Fetisov Yu. K. 《Technical Physics Letters》2020,46(5):487-490
Technical Physics Letters - The magnetoelectric (ME) effect in a planar amorphous ferromagnet–piezoelectric lead zirconate titanate (PZT) composite structure can be effectively excited by... 相似文献
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A new constitutive equation of thermoelasticity for crystals is presented based on the interatomic potential and solid mechanics at finite temperature. Using the new constitutive equation, the calculations for crystal copper and graphene are carried out under different loading paths at different temperatures. The calculated results are in good agreement with those of the previous thermoelasticity constitutive equation based on quantum mechanics, which clearly indicates that our new constitutive equation of thermoelasticity is correct. A lot of comparisons also show that the present theory is more concise and efficient than the previous thermal stress theory in the practical application. 相似文献
880.