Search Results - "Nitta, Aiko"
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Bioceramics Enhance the Anti-Tumor Activity of Immune Cells in Adoptive Immunotherapy
Published in International journal of molecular sciences (01-10-2024)“…Recent research has focused on immunotherapy with no side effects as an innovative medical treatment for cancer. However, typical drugs for immunotherapy are…”
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Discovery and structure–activity relationship of 2,6-disubstituted pyrazines, potent and selective inhibitors of protein kinase CK2
Published in Bioorganic & medicinal chemistry letters (01-07-2012)“…We report the discovery and structure–activity relationship of 2,6-disubstituted pyrazines, which are potent and selective CK2 inhibitors. Lead compound 1 was…”
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(3 R)-3-Amino-4-(2,4,5-trifluorophenyl)- N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Published in Bioorganic & medicinal chemistry (15-10-2008)“…Novel series of 3-amino- N-(4-aryl-1,1-dioxothian-4-yl)butanamides and 3-amino- N-(4-aryltetrahydropyran-4-yl)butanamides were synthesized and evaluated as…”
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Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors
Published in Bioorganic & medicinal chemistry letters (01-12-2012)“…A series of novel 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides were investigated as dipeptidyl peptidase IV (DPP-4) inhibitors. Introduction of a…”
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HIS-388, a novel orally active and long-acting 11β-hydroxysteroid dehydrogenase type 1 inhibitor, ameliorates insulin sensitivity and glucose intolerance in diet-induced obesity and nongenetic type 2 diabetic murine models
Published in The Journal of pharmacology and experimental therapeutics (01-10-2014)“…11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is considered a potential therapeutic target in the treatment of type 2 diabetes mellitus. In this study, we…”
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Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1
Published in Bioorganic & medicinal chemistry letters (15-03-2013)“…A series of novel 5-trans-hydroxyadamantan-2-yl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-ones that inhibit 11beta-hydroxysteroid dehydrogenase type 1 are…”
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Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists
Published in Bioorganic & medicinal chemistry letters (15-11-2012)“…Optimization starting with our lead compound 1 (IC50=4.9nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward…”
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Discovery and structure–activity relationships of urea derivatives as potent and novel CCR3 antagonists
Published in Bioorganic & medicinal chemistry letters (01-08-2012)“…The synthesis and structure–activity relationships of ureas as CCR3 antagonists are described. Optimization starting with lead compound 2 (IC50=190nM) derived…”
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Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition
Published in Bioorganic & medicinal chemistry (15-09-2008)“…The 6-fluoro-2-naphthylmethyl derivatives were prepared, and their inhibitory activities against CCR3 and CYP2D6 were evaluated. In our previous study on…”
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Synthesis, biological evaluation, and metabolic stability of acrylamide derivatives as novel CCR3 antagonists
Published in Bioorganic & medicinal chemistry (15-08-2009)“…Acrylamide derivatives were prepared, and their inhibitory activity against CCR3 and in vitro metabolic stability against human liver microsomes (HLMs) were…”
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Synthesis and structure–activity relationships of N-{1-[(6-fluoro-2-naphthyl)methyl]piperidin-4-yl}benzamide derivatives as novel CCR3 antagonists
Published in Bioorganic & medicinal chemistry (2008)“…The 6-fluoro-2-naphthylmethyl derivatives were prepared, and their inhibitory activities against CCR3 were evaluated. A novel class of potent CCR3 receptor…”
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