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Synthesis and Evaluation of Organosilicon Inhibitors of Active Purine Transport in Human Osteoblasts

In the search for new compounds that might, once incorporated into biomaterials, stimulate the natural processes of bone regeneration, a new series of silicon‐containing alkyl nucleobase analogues has been synthesized. An active hypoxanthine transport process in human osteoblasts was demonstrated, with an apparent Michaelis constant of 2.3 μM and a maximum possible rate of 0.47 pmol s−1×106 cell. The synthesized analogues were tested for toxicity in human osteoblasts. Nontoxic analogues were tested in competition transport studies with [14C]hypoxanthine. Two of them were found to inhibit the active transport of hypoxanthine in human osteoblasts, with IC50 values of 6.5 and 11.6 μM.