Zobrazeno 1 - 10 of 41 pro vyhledávání: '"Akihiro Tasaka"'
2
Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: Effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys
Autor: Masami Kusaka, Junzo Takahashi, Masuo Yamaoka, Satoru Asahi, Takahito Hara, Takenori Hitaka, Tomohiro Kaku, Toshiyuki Takeuchi, Hiroshi Miki, Akihiro Tasaka
Publikováno v: The Journal of Steroid Biochemistry and Molecular Biology. 129:115-128
Surgical or pharmacologic methods to control gonadal androgen biosynthesis are effective approaches in the treatment of a variety of non-neoplastic and neoplastic diseases. For example, androgen ablation and its consequent reduction in circulating le
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e25cb51d6b392d67dbb96e8b943c392
https://doi.org/10.1016/j.jsbmb.2012.01.001
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3
Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer
Autor: Nobuyuki Matsunaga, Akihiro Tasaka, Satoru Asahi, Mari Adachi, Takahito Hara, Toshimasa Tanaka, Teruaki Okuda, Akio Ojida, Takenori Hitaka, Shuichi Furuya, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
Publikováno v: Bioorganic & Medicinal Chemistry. 19:6383-6399
A novel naphthylmethylimidazole derivative 1 and its related compounds were identified as 17,20-lyase inhibitors. Based on the structure–activity relationship around the naphthalene scaffold and the results of a docking study of 1a in the homology
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d9ae1020bfeecd91e9f7d00f654b7c3
https://doi.org/10.1016/j.bmc.2011.08.066
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4
17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure–activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors
Autor: Toshimasa Tanaka, Saori Tsujimoto, Tomohiro Kaku, Masuo Yamaoka, Akihiro Tasaka, Masami Kusaka, Nobuyuki Matsunaga, Takahito Hara
Publikováno v: Bioorganic & Medicinal Chemistry. 19:2428-2442
A novel series of biphenylylmethylimidazole derivatives and related compounds were synthesized as inhibitors of 17,20-lyase, a key enzyme in the production of steroid hormones, and their biological activities were evaluated. In an attempt to identify
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f00b6983c19e8de9a9dd65127d0511aa
https://doi.org/10.1016/j.bmc.2011.02.009
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5
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I
Autor: Takahito Hara, Mitsuru Shiraishi, Junichi Miyazaki, Akihiro Tasaka, Masuo Yamaoka, Takenori Hitaka, Toshio Miyawaki, Katsuji Aikawa, Naoyuki Kanzaki, Masami Kusaka, Satoshi Yamamoto, Yumi N. Imai
Publikováno v: Bioorganicmedicinal chemistry. 23(10)
To develop effective drugs for hypogonadism, sarcopenia, and cachexia, we designed, synthesized, and evaluated selective androgen receptor modulators (SARMs) that exhibit not only anabolic effects on organs such as muscles and the central nervous sys
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59e2cc5819a7323d675f18b5607c7a37
https://pubmed.ncbi.nlm.nih.gov/25862209
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6
C17,20-lyase inhibitors. Part 2: Design, synthesis and structure–activity relationships of (2-naphthylmethyl)-1H-imidazoles as novel C17,20-lyase inhibitors
Autor: Nobuyuki Matsunaga, Masuo Yamaoka, Takahito Hara, Akihiro Tasaka, Toshimasa Tanaka, Tomohiro Kaku, Akio Ojida, Masami Kusaka
Publikováno v: Bioorganic & Medicinal Chemistry. 12:4313-4336
A series of 1- and 4-(2-naphthylmethyl)-1H-imidazoles (3 and 4) has been synthesized and evaluated as C17,20-lyase inhibitors. Several 6-methoxynaphthyl derivatives showed potent C17,20-lyase inhibition, suppression of testosterone biosynthesis in ra
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5f29737929a447a9d54b77ba2eddaff
https://doi.org/10.1016/j.bmc.2004.06.016
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7
Synthetic studies on (1S)-1-(6,7-dimethoxy-2-naphthyl)-1-(1H-imidazol-4-yl)-2-methylpropan-1-ol as a selective C17,20-lyase inhibitor
Autor: Nobuyuki Matsunaga, Akio Ojida, Akihiro Tasaka, Tomohiro Kaku
Publikováno v: Tetrahedron: Asymmetry. 15:2021-2028
An asymmetric synthesis of the selective C 17,20 -lyase inhibitor 2 has been established in eight steps from 2,3-dihydroxynaphthalene 9 . The key steps are the enantioselective oxidation of ketone 17 to the chiral α-hydroxy ketone 18 and the diaster
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6a8e1e04a65d4c83d24d0697e3c71260
https://doi.org/10.1016/j.tetasy.2004.05.044
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8
C17,20-Lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors
Autor: Masahiko Iwasaki, Masuo Yamaoka, Nobuyuki Matsunaga, Takahito Hara, Toshimasa Tanaka, Masami Kusaka, Tetsuya Aono, Akihiro Tasaka, Tomohiro Kaku, Fumio Itoh, Hiroshi Miki
Publikováno v: Bioorganic & Medicinal Chemistry. 12:2251-2273
Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds exhibited potent C(17,20)-lyase inhibition. However, in vivo activities were found to be sh
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d9854d7fc1f1b0b27a638b08d8a76ce
https://doi.org/10.1016/j.bmc.2004.02.007
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9
Stereocontrolled synthesis of (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methylpropan-1-ol as a potent C17,20-lyase inhibitor
Autor: Akio Ojida, Akihiro Tasaka, Nobuyuki Matsunaga, Tomohiro Kaku
Publikováno v: Tetrahedron: Asymmetry. 15:1555-1559
An efficient stereocontrolled synthesis of the potent C17,20-lyase inhibitor, (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methyl-1-propanol 1, has been established. The stereogenic center of 1 was successfully constructed by a highly diaster
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::40bfc74f8b2d313ed966c6fbb27b7d38
https://doi.org/10.1016/j.tetasy.2004.02.035
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10
Total Synthesis of (−)-Bafilomycin A1
Autor: William R. Roush, Karl A. Scheidt, Brad M. Savall, Glenn J. Fegley, Michael D. Wendt, Thomas D. Bannister, Akihiro Tasaka
Publikováno v: Journal of the American Chemical Society. 124:6981-6990
A highly stereoselective total synthesis of (-)-bafilomycin A(1), the naturally occurring enantiomer of this potent vacuolar ATPase inhibitor, is described. The synthesis features the highly stereoselective aldol reaction of methyl ketone 8b and alde
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9834088852ce32140d2c15435e825b0
https://doi.org/10.1021/ja017885e
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