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Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.
Total synthesis of human chymase inhibitor methyllinderone has been achieved in only four steps with an overall yield of 21% from dimethyl squarate. We developed an efficient synthetic method forExpand
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Bisindolylmaleimide I and V inhibit necrosis induced by oxidative stress in a variety of cells including neurons
Although free radical-mediated necrosis is implicated in many diseases such as neurodegeneration, potent anti-necrotic drugs have not yet been exploited. We found that bisindolylmaleimide I (BMI orExpand
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A steroidogenic cell line with differentiation potential from mouse granulosa cells, transfected with Ad4BP and SV40 large T antigen genes.
Several steroidogenic cell lines of granulosa cells (GC) have been used to elucidate differentiation mechanisms of GC during folliculogenesis. These cell lines, however, are of limited usefulnessExpand
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A practical method for oxazole synthesis by cycloisomerization of propargyl amides.
[reaction: see text] 2,5-disubstituted and 2,4,5-trisubstituted oxazol-5-yl carbonyl compounds were prepared in good yields by a mild SiO2-mediated cycloisomerization of propargyl amides.
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Protein kinase C-dependent down-regulation of basic fibroblast growth factor (FGF-2) receptor by phorbol ester and epidermal growth factor in porcine granulosa cells.
The regulation of the basic fibroblast growth factor (bFGF, or FGF-2) receptor on porcine granulosa cells was studied. Receptor levels before and after cell differentiation in vivo and in vitro didExpand
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Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors.
3-Benzylazetidine-2-one derivatives were designed and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23, whichExpand
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1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure-activity relationship studies of 1-oxacephems led to compounds 15, which exhibited 27 nM inhibition ofExpand
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Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 1-oxacephems led to compound 34, which exhibited 6 nMExpand
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Development of Safe One-Pot Synthesis of N-1- and C-2-Substituted Benzimidazole via Reductive Cyclization of o-Nitroarylamine Using Na2S2O4
We report that the reductive cyclization of o-nitroarylamine with aldehyde using sodium dithionite (Na2S2O4) could be accelerated by addition of H2O, which made it possible to control the heatExpand
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