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What kinds of substrates show P-glycoprotein-dependent intestinal absorption? Comparison of verapamil with vinblastine.
The influence of P-glycoprotein (P-gp) on intestinal absorption of drugs was investigated by comparison of the uptakes of two P-gp substrates, verapamil and vinblastine, using intestinal segments of
Antitumor activity of shikonin and its derivatives.
Shikonin, a naphthoquinone contained in the root of Lithospermum officinalis var. erythrorhizon MAX. and Macrotomia euchroma (ROYLE) PAULS (Boraginaceae), showed a high antitumor activity against the
Studies on novel bone resorption inhibitors. II. Synthesis and pharmacological activities of fused aza-heteroarylbisphosphonate derivatives.
Two new series of fused aza-heteroarylbisphosphonates (5, 8), which are structurally quite different from incadronate (YM175), and related compounds were synthesized and evaluated for antiresorptive
Peptide based interleukin-1 beta converting enzyme (ICE) inhibitors: synthesis, structure activity relationships and crystallographic study of the ICE-inhibitor complex.
TLDR
Compound 27c is the first example that shows a strong inhibitory activity without the carboxyl group at the P1 position, and dose dependently inhibited LPS-primed ATP-induced IL-1 beta release in mice.
Studies on novel bone resorption inhibitors. I. Synthesis and pharmacological activities of aminomethylenebisphosphonate derivatives.
TLDR
(cycloheptylamino)methylenebis(phosphonic acid) (3j) was finally selected for further investigation, proving 10-fold as potent as pamidronate in the PIH model and an immobilization bone atrophy model in rats (DA model).
One-Pot Preparation of 1-Substituted Imidazole-2-thione from Isothiocyanate and Amino Acetal
Abstract Isothiocyanates were treated with amino acetal and conc. HCl (0.5 eq.) successively in one-pot to afford 1-substituted imidazole-2-thiones in good yields.
Alternative Synthesis of Dibenzo-and Dipyrido-[1,3]Diazepines from Thioamides and o,o′-Diaminobiaryls
Abstract Thioamides were treated with iodomethane, and then o,o′-diaminobiphenyl or bipyridyl to afford 6-substituted-5H-dibenzo- or dipyrido [1,3]diazepines in good yields.
Stereoselectivity of a potent calcium antagonist, 1-benzyl-3-pyrrolidinyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
Four enantiomers (3a-d) of the title compound, YM-09730 (3), were synthesized by the reaction of (-)- or (+)-5-(methoxycarbonyl)-2, 6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid
Studies on aromatase inhibitors. I. Synthesis and biological evaluation of 4-amino-4H-1,2,4-triazole derivatives.
TLDR
The data suggest that YM511 is a highly selective aromatase inhibitor and may be a useful agent for the treatment of estrogen-dependent diseases such as breast cancer.
Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).
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