Diastereomeric and geometric analogs of calcipotriol, PRI-2202 and PRI-2205, were synthesized as advanced intermediates from vitamin D C-22 benzothiazoyl sulfones and side-chain aldehydes using our convergent strategy. Calcitriol, calcipotriol (PRI-2201) and tacalcitol (PRI-2191) were used as the reference compounds. Among a series of tested analogs the diastereomeric analog PRI-2202 showed the strongest antiproliferative activity on the human breast cancer cell line MCF-7, whereas the geometric analog PRI-2205 was the weakest. Both analogs were less potent in antiproliferative activity against HL-60 cells compared to the reference compounds. The ability to potentiate antiproliferative effect of cisplatin or doxorubicin against HL-60 cells or that of tamoxifen against the MCF-7 cell line was observed at higher doses of PRI-2202 or PRI-2205 than those of the reference compounds. The proapoptotic activity of tamoxifen, expressed as the diminished mitochondrial membrane potential, as well as the increased phosphatidylserine expression, was partially attenuated by calcitriol, PRI-2191, PRI-2201 and PRI-2205. The treatment of the MCF-7 cells with tamoxifen alone resulted in an increase in VDR expression. Moreover, a further increase in VDR expression was observed when the analogs PRI-2201 or PRI-2205, but not PRI-2191, were used in combination with tamoxifen. This observation could partially explain the potentiation of the antiproliferative effect of tamoxifen by vitamin D analogs.

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This study investigated the possibility of applying flat-pressed wood-polymer composites in conditions of high humidity. The experiment involved three variants of wood-polymer composite panels 16 mm thick, and 680 kg per m3 density. The wood particles were bonded with polyethylene. The share of polyethylene in the core layer was fixed at 50%, while in the face layers the content was varied (40%, 50%, or 60%). The following parameters were examined: modulus of rupture (MOR), modulus of elasticity (MOE), internal bond (IB), screw holding (SH), thickness swelling (TS), water absorption (WA), susceptibility to drilling and milling, wettability and surface free energy, and resistance to mold. The results were compared to particleboard glued with urea-formaldehyde resin. The wood-polymer composite had lower MOR and MOE values and similar IB and SH values. The panels indicated a remarkably higher water resistance (lower TS and WA values) with good surface wettability and high resistance to mold fungi. Additionally, the composites were easier to machine, e.g. drilling or milling, in comparison to standard particleboards.

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