Design, synthesis and in vitro evaluation of amidoximes as histone deacetylase inhibitors for cancer therapy.

Amindoximes are geometric isomers of N-hydroxyamidines which are bioisosteres of hydroxamates. Since amindoxime group is capable of chelating transition metal ions including zinc ion, amindoximes should possess histone deacetylases (HDACs) inhibitory activity. In this work, we designed and synthesized a series of amindoximes, examined their inhibitory activities against HDACs, and investigated their cytotoxicity to human cancer cells. Preliminary results demonstrated that amindoximes possessed submicromolar HDACs inhibitory activity, with noteworthy enhancement compared with hydroxamates. Furthermore, the amindoximes arrested HCT116 and A549 cells in G2/M phase and showed good efficacy in inducing cells death. We provided a proof-of-concept that amindoximes could be used as HDACs inhibitors and hold great promise as epigenetic drugs.

A Fixed-Time Noise-Tolerance ZNN Model for Time-Variant Inequality-Constrained Quaternion Matrix Least-Squares Problem.

Presently, numerical algorithms for solving quaternion least-squares problems have been intensively studied and utilized in various disciplines. However, they are unsuitable for solving the corresponding time-variant problems, and thus few studies have explored the solution to the time-variant inequality-constrained quaternion matrix least-squares problem (TVIQLS). To do so, this article designs a fixed-time noise-tolerance zeroing neural network (FTNTZNN) model to determine the solution of the TVIQLS in a complex environment by exploiting the integral structure and the improved activation function (AF). The FTNTZNN model is immune to the effects of initial values and external noise, which is much superior to the conventional zeroing neural network (CZNN) models. Besides, detailed theoretical derivations about the global stability, the fixed-time (FXT) convergence, and the robustness of the FTNTZNN model are provided. Simulation results indicate that the FTNTZNN model has a shorter convergence time and superior robustness compared to other zeroing neural network (ZNN) models activated by ordinary AFs. At last, the construction method of the FTNTZNN model is successfully applied to the synchronization of Lorenz chaotic systems (LCSs), which shows the practical application value of the FTNTZNN model.

Bio-inspired immobilization of metal oxides on monolithic microreactor for continuous Knoevenagel reaction.

A facile method is reported to construct monolithic microreactor with high catalytic performance for Knoevenagel reaction. The microreactor is based on hierarchically porous silica (HPS) which has interconnected macro- and mesopores. Then the HPS is surface modified by pyrogallol (PG) polymer. Al(NO3)3 and Mg(NO3)2 are loaded on the surface of HPS through coordination with -OH groups of PG. After thermal treatment, Al(NO3)3 and Mg(NO3)2 are converted Al2O3 and MgO. The as-synthesized catalytic microreactor shows a high and stable performance in Knoevenagel reaction. The microreactor possess large surface area and interconnected pore structures which are beneficial for reactions. Moreover, this economic, facile and eco-friendly surface modification method can be used in loading more metal oxides for more reactions.