Search Results - "Takenouchi, Kazuya"
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Development of 14-epi-19-Nortachysterol and Its Unprecedented Binding Configuration for the Human Vitamin D Receptor
Published in Journal of the American Chemical Society (11-05-2011)“…In the study of the synthesis of 14-epi-19-norprevitamin D3, we found 14-epi-19-nortachysterol derivatives through C6,7-cis/trans isomerization. We also…”
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Synthesis and Biological Activities of 1α,4α,25- and 1α,4β,25-Trihydroxyvitamin D3 and Their Metabolism by Human CYP24A1 and UDP-Glucuronosyltransferase
Published in Chemical & pharmaceutical bulletin (01-10-2012)“…A previous report has demonstrated the existence of a C4-hydroxylated vitamin D2 metabolite in serum of rats treated with pharmacological doses of vitamin D2…”
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Synthesis and Biological Evaluation of 4-Substituted Vitamin D and 14-Epi-Previtamin D Analogs
Published in Chemical & Pharmaceutical Bulletin (01-12-2009)“…We synthesized the 4-hydroxy and 4-methoxy analogs of active vitamin D3 (1α,25(OH)2D3, 1) and its C14-epimer with the previtamin D3 form of…”
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Structure–activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist
Published in Bioorganic & medicinal chemistry (01-08-2008)“…Structure–activity relationship studies on 1α,25-dihydroxyvitamin D 3-26,23-lactams (DLAMs), antagonists of vitamin D, were conducted, focusing on the…”
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Synthesis and Biological Activities of 14-epi-MART-10 and 14-epi-MART-11: Implications for Cancer and Osteoporosis Treatment
Published in Anticancer research (01-09-2009)“…The 14-epimer of MART-10, namely 14-epi-MART-10 (14-epi-2α-(3-hydroxypropyl)-1α,25-dihydroxy-19-norvitamin D 3 ) and its 2-epimeric analog (14-epi-MART-11)…”
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Journal Article Conference Proceeding -
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Creative synthesis of novel vitamin D analogs for health and disease
Published in Journal of steroid biochemistry and molecular biology (01-03-2007)“…We report new analogs of 1α,25-dihydroxyvitamin D3 (1) in three categories. First, design and synthesis of ligands for a mutant vitamin D receptor…”
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Journal Article Conference Proceeding -
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Synthesis and Biological Activities of 1α,4α,25- and 1α,4β,25-Trihydroxyvitamin D3 and Their Metabolism by Human CYP24A1 and UDP-Glucuronosyltransferase
Published in Chemical and Pharmaceutical Bulletin (01-10-2012)“…A previous report has demonstrated the existence of a C4-hydroxylated vitamin D2 metabolite in serum of rats treated with pharmacological doses of vitamin D2…”
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Synthesis and structure-activity relationships of TEI-9647 derivatives as Vitamin D3 antagonists
Published in Journal of steroid biochemistry and molecular biology (01-05-2004)“…The Vitamin D(3) lactone analogues, (23S)- and (23R)-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactone (TEI-9647 and TEI-9648) are antagonists of the…”
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Conference Proceeding Journal Article -
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Synthesis and 2a-Modification of 24-Phenylvitamin D3 Lactones: Effects on VDR Antagonistic Activity
Published in Heterocycles (2006)Get full text
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Vitamin D and cancer
Published in Clinical calcium (01-07-2006)“…Vitamin D is a steroid hormone which regulates calcium and bone homeostasis through intestine, bone, kidney and parathyroid. It has been reported that vitamin…”
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Synthesis and biological activities of vitamin D3 derivatives with cyanoalkyl side chain at C-2 position
Published in The Journal of steroid biochemistry and molecular biology (01-04-2015)“…•We synthesized vitamin D3 derivatives with cyanoalkyl side chain at C-2 position.•These novel derivatives showed strong transactivation activities.•Nitrogen…”
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Design and synthesis of 2α-(tetrazolylethyl)-1α,25-dihydroxyvitamin D3 as a high affinity ligand for vitamin D receptor
Published in The Journal of steroid biochemistry and molecular biology (01-10-2014)“…•We synthesized 2α-heteroarylethyl active vitamin D3 for SAR study.•The 2α-[2-(tetrazol-2-yl)ethyl] group enhanced transactivation activity.•X-ray…”
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Synthesis of 14-epi-2α-hydroxypropoxy-1α,25-dihydroxy-19-nortachysterol and its hVDR binding
Published in The Journal of steroid biochemistry and molecular biology (01-07-2013)“…▸ We synthesized a new stable 14-epi-19-nortachysterol derivative. ▸ We tested hVDR binding affinity of the 2α-substituted analog. ▸ The 2α-(3-hydroxypropoxy)…”
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Synthesis of C-2 substituted vitamin D derivatives having ringed side chains and their biological evaluation, especially biological effect on bone by modification at the C-2 position
Published in Organic & biomolecular chemistry (21-05-2011)“…In order to obtain vitamin D derivatives, which have strong activity for enhancing bone growth, we designed vitamin D derivatives with various substitutions at…”
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Synthesis of novel C-2 substituted vitamin D derivatives having ringed side chains and their biological evaluation on bone
Published in The Journal of steroid biochemistry and molecular biology (01-07-2013)“…▸ We synthesized novel vitamin D3 derivatives with chiral cyclopentanone in the side chain. ▸ Novel derivatives showed strong transactivation activities in…”
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Synthesis of 2α-Heteroarylalkyl Active Vitamin D3 with Therapeutic Effect on Enhancing Bone Mineral Density in Vivo
Published in ACS medicinal chemistry letters (11-07-2013)“…2α-Heteroarylethyl-1α,25-dihydroxyvitamin D3 analogues, which were designed to form a hydrogen bond between Arg274 of human vitamin D receptor (hVDR) and a…”
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Synthesis of 2α-Heteroarylalkyl Active Vitamin D 3 with Therapeutic Effect on Enhancing Bone Mineral Density in Vivo
Published in ACS medicinal chemistry letters (11-07-2013)Get full text
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Synthesis of 2α- and 2β-substituted-14- epi-previtamin D 3 and their genomic activity
Published in Tetrahedron (17-07-2010)“…2α- and 2β-Substituted analogs of 14- epi-previtamin D 3 were synthesized and isolated after thermal isomerization of 14- epi-vitamin D 3 triene at 80 °C. The…”
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New C15-Substituted Active Vitamin D3
Published in Organic letters (03-06-2011)“…C15-Substituted 1α,25-dihydroxyvitamin D3 analogs were synthesized for the first time to investigate the effects of the modified CD-ring on biological activity…”
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