Zobrazeno 1 - 10
of 54
pro vyhledávání: '"Masao Nagaoka"'
Publikováno v:
Steroids. 74:884-889
Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New 6beta,19-bridged steroid analogs of androstenedione, 6beta,19-epithio- and 6beta,19-methano compounds 11 and 17, were synthesized starting from 19
Publikováno v:
Steroids. 73:1262-1269
Inhibition of aromatase activity in human placental microsomes with androstenedione (AD) (1a) and its 19-oxygenated derivatives 1b and 1c, their 16alpha-hydroxy compounds 2 and 3, and 3-deoxyandrost-4-ene compounds 5 and 6 was studied using [1beta-(3
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 107:211-219
To gain insight into the mechanistic features for aromatase inactivation by the typical suicide substrates, androsta-1,4-diene-3,17-dione (ADD, 1) and its 6-ene derivative 2, we synthesized 19-substituted (methyl and halogeno) ADD and 1,4,6-triene de
Autor:
Masao Nagaoka, Mitsuteru Numazawa
Publikováno v:
Steroids. 70:831-839
Aromatase is a cytochrome P-450 enzyme complex that catalyzes the conversion of androst-4-ene-3,17-dione (AD) to estrone through three sequential oxidations of the 19-methyl group. 3-DeoxyAD ( 1 ) and its 5-ene isomer 4 are potent and good competitiv
Publikováno v:
東北薬科大学研究誌. 51:23-29
Aromatase is a cytochrome P-450 enzyme responsible for the conversion of androgens to estrogens. 2,2-Dimethylandrostenedione (5) is one of the powerful inhibitors of the enzyme. To explore a metabolic switching in the aromatase-catalyzed biotransform
Publikováno v:
Chemical and Pharmaceutical Bulletin. 52:722-726
To study the stereochemical aspects of the aromatase reaction of androst-4-en-17-one (1) and its 5-ene isomer 4, competitive inhibitors of aromatase, the [19S-(3)H]- and [19R-(3)H]-labeled 19-hydroxy derivatives 2 and 5, were synthesized through NaB(
Autor:
Yasuyo Muroi, Yoko Watari, Kaoru Tsukioka, Hiromi Yajima, Mitsuteru Numazawa, Masao Nagaoka, Keiko Yamada
Publikováno v:
Steroids. 68:533-542
As part of our investigation into the structure–activity relationship of a novel class of aromatase inhibitors, two series of 3-deoxy androgens, androst-5-en-17-ones with a non-polar alkoxy ( 5 and 6 ), alkyl ( 20 − 22 ), or phenylalkyl ( 23 and
Publikováno v:
Chemical and Pharmaceutical Bulletin. 48:1215-1218
16Alpha-hydroxy-17-keto steroids, 1, 3, and 8, and their 17beta-hydroxy-16-keto isomers, 4, 5, and 9, were transformed into the corresponding 17beta-alkoxy-16-keto derivatives on treatment with trimethylsilyl iodide (TMSI) in the presence of alkyl al
Publikováno v:
Chemical and Pharmaceutical Bulletin. 47:548-553
Deoxygenation reaction of steroidal 16,17-ketols 1, 2 and 6 as well as their silyl ethers 3 and 7 and 16- and 17-iodoketone analogs 11, 12, and 14 with trimethylsilyl iodide (TMSI) or HI under various conditions was examined. The results indicate tha
Publikováno v:
Chemical and Pharmaceutical Bulletin. 47:263-266
[3β, 7, 7, 17α-2H4]Androst-5-ene-17β, 19-diol (6) and [3, 3, 7, 7, -2H4]androst-4-ene-17β, 19-diol (15-d4) were synthesized as internal standards for gas chromatographic-mass spectrometric analysis of the 19-hydroxylation of androst-5-en-17-one (