Novel silicon-containing drugs derived from the indomethacin scaffold: Synthesis, characterization and evaluation of biological activity

Synthesis, spectroscopic characterization and in vitro pharmacological and cancer cell growth inhibitory activity studies of new silicon-containing compounds based on the indomethacin scaffold are now reported. Amidation of the indomethacin carboxylate group using amino-functional silanes generated a series of novel lipophilic derivatives of indomethacin. The pharmacological activity of these derivatives tested against human recombinant cyclooxygenase-1 and 2 demonstrated that the silicon-containing derivatives are cyclooxygenase-2 (COX-2) selective. The silicon-containing amides of indomethacin demonstrated in vitro growth inhibitory activity against human MiaPaCa-2 pancreatic carcinoma cells at low μM concentrations. The 3a and 3c derivatives exhibited the most potent in vitro antiproliferative activity, with IC₅₀ <6.0 μM, compared to unmodified indomethacin having an IC₅₀100 μM. We dedicate this paper to Prof. Mitsuo Kira, outstanding organosilicon chemist and valued friend.     

Summary of ISO/TC 201 Standard: X ISO 17560:2002—Surface chemical analysis—Secondary ion mass spectrometry—Method for depth profiling of boron in silicon

This International Standard specifies a secondary ion mass spectrometric method using magnetic‐sector or quadrupole mass spectrometers for depth profiling of boron in silicon, and using stylus profilometry or optical interferometry for depth calibration. This method is applicable to single‐crystal, polycrystal or amorphous silicon specimens with boron atomic concentrations between 1 × 10¹⁶ and 1 × 10²⁰ atoms cm^?3, and to the crater depth of 50 nm or deeper. Optical interferometry is generally applicable to crater depths in the range 0.5–5 µm. Copyright © 2004 John Wiley & Sons, Ltd.     

Anchoring transitions of liquid crystals on SiO x

Anchoring transitions were observed of nematic liquid crystal (LC) mixtures on obliquely evaporated SiO _x by varying the relative abundance of two components in the mixture. Of these two components, one has a longitudinal cyano group and another has lateral cyano groups. It was also found that both temperature and SiO _x thickness variations are able to shift the anchoring transitions. The anchoring on SiO _x has two origins: long‐range van der Waals potential and short‐range surface interactions. Since the two origins have opposite preference in LC director orientation the observed transition is caused by the change of their relative strength. Thermal absorption–desorption of molecules on SiO _x surface is important in determining the strength of short‐range interactions, whereas the layer thickness and optical properties of SiO _x are dependent on the van der Waals potential. Based on previous work by de Gennes we propose a model to describe the observed phenomenon.