Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Akihiro TASAKA"'
Publikováno v:
AEROSPACE TECHNOLOGY JAPAN, THE JAPAN SOCIETY FOR AERONAUTICAL AND SPACE SCIENCES. 12:25-30
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
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
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
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
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
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
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
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
Autor:
Tomohiro Kaku, Hitomi Yamasaki, Naohiro Kawaguchi, Masami Kusaka, Akihiro Tasaka, Masuo Yamaoka, Toshiyuki Takeuchi, Takenori Hitaka, Hiroshi Miki, Takahito Hara
Publikováno v:
Cancer Research. 70:DD01-03
Background: Recent studies suggest that residual adrenal androgen after castration could be responsible for the progression of castration-resistant prostate cancer (CRPC). To develop an effective therapy for CRPC that inhibits the production of adren