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Here, we present a new series of hydrazide-bearing class I selective HDAC inhibitors designed based on panobinostat. The cap, linker, and zinc-binding group were derivatized to improve HDAC affinity and antileukemia efficacy. Lead inhibitor 13a shows picomolar or low nanomolar IC50 values against HDAC1 and HDAC3 and exhibits differential toxicity profiles toward multiple cancer cells with different FLT3 and p53 statuses. 13a indirectly inhibits the FLT3 signaling pathway and down-regulates master antiapoptotic proteins, resulting in the activation of pro-caspase3 in wt-p53 FLT3-ITD MV4-11 cells. While in the wt-FLT3 and p53-null cells, 13a is incapable of causing apoptosis at a therapeutic concentration. The MDM2 antagonist and the proteasome inhibitor promote 13a-triggered apoptosis by preventing p53 degradation. Furthermore, we demonstrate that apoptosis rather than autophagy is the key contributing factor for 13a-triggered cell death. When compared to panobinostat, 13a is not mutagenic and displays superior in vivo bioavailability and a higher AUC0-inf value.This work presents an improvement in the activity and catalytic lifetime of Pt deposits on Bi-modified Pt nanoparticles (Bi/Pt NP) toward formic acid oxidation (FAO). Using an irreversible adsorption method, Bi was deposited on Pt NP to form Bi/Pt NP and sequentially Pt was deposited on Bi/Pt NP to form Pt/Bi/Pt NP. Voltammetric studies of Pt NP, Bi/Pt NP, and Pt/Bi/Pt NPs supported that Pt deposits of Pt/Bi/Pt NPs provided quite a unique behavior simultaneous surface oxidation of deposited Pt and Bi and significant resistance to the oxidative removal of Bi. Furthermore, combined spectroscopic investigations revealed that the concentration of the employed Pt precursor ion solution determined the amount of deposited Pt from ∼0.2 to ∼0.4 in coverage. The best Pt/Bi/Pt NP catalyst with a Pt coverage of ∼0.25 enhanced the dehydrogenation processes below ∼0.4 V by a factor of more than 2 and increased the FAO current at ∼0.8 V roughly by 15 times, referring to those of Bi/Pt NP. The lifetime measurement works revealed that after the 1000th voltammetric cycle to 0.4 V, the FAO currents of Pt/Bi/Pt NPs were 2 and 4 times higher than those of Bi/Pt NP and Pt NP, respectively. The Pt deposits on Bi/Pt NP were concluded to play two roles in FAO the promotion of FAO processes to increase the activity and the retardation of Bi oxidative removal to maintain the activity much longer.We investigated the potential for waterless urinal sealants fluids to remove pharmaceuticals from urine. 1H NMR, FTIR, and GC/MS characterization of the fluids indicated that they are mostly composed of aliphatic compounds. Removal of ethinyl estradiol was >40% for two of the three sealant fluids during simulated urination to a urinal cartridge but removal of seven other compounds with greater hydrophilicity was 3.5. At equilibrium with synthetic urine, removal ranged widely from 2% to 100%. Kow was poorly correlated with removal for both matrices at equilibrium, but Dow was correlated with removal from synthetic urine for two of the three sealants, indicating that ionization and hydrophilicity control partitioning between the urine and sealant phases. To improve removal during urination, where equilibrium is not achieved, we increased the hydraulic retention time 100-fold over that of typical male urination. Removal of specific hydrophobic compounds increased, indicating that both hydrophobicity and kinetics control removal. Removal of ethinyl estradiol was ≥90% for all sealants in the increased hydraulic retention time experiment, demonstrating the potential for implementation to female urinals.In the present study, the memristive characteristics of hydrothermally grown TiO2 nanorod arrays, particularly, the difference in the retention time of the resistance state, are investigated in dependence of the array growth temperature. A volatile behavior is observed and related to a redistribution of oxygen vacancies over time. It is shown that the retention time increases for increasing array growth temperatures from several seconds up to 20 min. The relaxation behavior is also seen in the current-voltage characteristics, which do not show the common unipolar, bipolar, or complementary switching behavior. Instead, the temporal evolution depends on the duration of the applied voltage and on the nanowire growth temperature. Therefore, electronic measurements are combined with scanning electron and scanning transmission electron microscopy, so that the amount of oxygen defect-rich grain boundaries in the upper part of the nanowires can be linked to the differences in the current-voltage behavior and retention time.High-valent chiral oxidovanadium(V) complexes derived from 3,5-substituted-N-salicylidene-l-tert-leucine were used as catalysts in asymmetric reduction of N-benzyl-β-ketoamides. check details Among six different solvents, three different alcohol additives, and two different boranes examined, the use of pinacolborane in tetrahydrofuran (THF) with a t-BuOH additive led to the best results at -20 °C. The corresponding β-hydroxyamides can be furnished with yields up to 92% and an enantiomeric excess (ee) up to 99%. We have successfully extended this catalytic protocol for the synthesis of an (S)-duloxetine precursor.Single-molecule conductance of a B-N substituted phenanthrene derivative and its isoelectronic C═C counterpart was investigated by the scanning tunneling microscopy break junction (STM-BJ) technique. The incorporation of the B-N motif results in a better single-molecule conductivity than the C═C analogue. Furthermore, the Lewis acid-base reaction between F- and the B atom of the B-N motif leads to a decrease of the conductance of the BN derivative, which can be understood due to the shifting of the energy positions of the LUMO, as revealed by quantum transport calculations, even though the HOMO-LUMO gap decreases in the B-F Lewis acid-base. These findings provide insights for modulating electron transport properties by isoelectronic structure design. The B-N isoelectronic substituted structure could be a feasible way to design single-molecule devices such as switches and chemical sensors.

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