The Effect of Vicinal Difluorination on the Conformation and Potency of Histone Deacetylase Inhibitors

Histone deacetylase enzymes (HDACs) are potential targets for the treatment of cancer and other diseases, but it is challenging to design isoform-selective agents. In this work, we created new analogs of two established but non-selective HDAC inhibitors. We decorated the central linker chains of the molecules with specifically positioned fluorine atoms in order to control the molecular conformations. The fluorinated analogs were screened against a panel of 11 HDAC isoforms, and minor differences in isoform selectivity patterns were observed.     

A comparison of clay colloid and artificial microsphere transport in natural discrete fractures

Transport of monodispersed buoyant 1-mum latex microspheres, dense 1.34-microm montmorillonite particles, Li(+) and Br(-) was investigated in a naturally fractured chalk core with an average equivalent hydraulic aperture of 183 microm. Studied parameters were: tracer arrival time, C/C(0) values, mass recovery, size distribution and the impact of initial concentration. Breakthrough time of both colloidal tracers was faster than that of the soluble tracers. Significantly lower recovery and slightly slower breakthrough time were observed for the clay particles relative to the microspheres, apparently mainly due to the former's higher density, resulting in preferential gravitational settling of the clay particles. However, variable surface charge and nonuniform shape and size of the clay particles may also play a role in the observed differences. From the theoretical scale ratio, the time interval calculation seems to be a major factor in colloid recovery. Clay-particle size fractionation was observed (0.62 vs 1.34 microm at the outflow and inflow, respectively), and there was no significant influence of the initial concentration (100 and 500 mg/L) on transport properties. Our observations indicate that colloid density is a dominant property for their transport in fractures. This work emphasizes the need for caution when the results of studies in which buoyant colloids are used as tracers are extrapolated to natural systems in which clay colloids are present.     

Interfacial characterisation and mechanical properties of heat treated non-woven kenaf fibre and its reinforced composites

This paper reports on the comprehensive characterisation of heat treated kenaf fibre (KF) and its composites. The kenaf fibres were modified by heating for 2.5–12.5 h inside a drying oven. Heat treatment produces an increase in the crystallinity index and fibre strength of KF. The highest value of KF strength was recorded by applying heat treatment of 10 h on KF. The heat treatment results in the partial removal of impurities/extractives on the KF surface which is detected by scanning electron microscopy and X-ray photoelectron spectroscopy. Atomic force microscopy results signify the decrease of roughness, the increase in peak area density and the increase of the adhesion force on the surface area of heat treated KF. The effect of the heat treatment in enhancing the interface bonding characteristics between the KF and unsaturated polyester matrix can be reflected by the interlaminar shear strength (ILSS) and dynamic mechanical analysis value of the composites. The flexural properties of the composites showed a similar trend to ILSS. However, the fracture toughness revealed contrasting results. Water absorption induced a drastic loss of the mechanical properties of the composites albeit better retention of properties was observed in the case of heat-treated KF composites.