Zobrazeno 1 - 10
of 37
pro vyhledávání: '"S.E. Barrie"'
Autor:
S.E. Barrie, Martin G. Rowlands, Ferdinand Chan, Michael Jarman, Ben P. Haynes, Gerard A. Potter, John Houghton
Publikováno v:
Journal of Medicinal Chemistry. 39:3319-3323
Various 3- and 4-pyridylalkyl 1-adamantanecarboxylates have been synthesized and tested for inhibitory activity toward the 17 alpha-hydroxylase and C17,20-lyase activities of human testicular cytochrome P450(17 alpha). The 4-pyridylalkyl esters were
Autor:
S.E. Barrie, Gerard A. Potter, Martin G. Rowlands, John Houghton, Raymond McCague, Ferdinand Chan, Michael Jarman
Publikováno v:
Journal of Medicinal Chemistry. 38:4191-4197
Esters of 3- and 4-pyridylacetic acid have been prepared and tested for inhibitory activity toward the human testicular 17 alpha-hydroxylase/C17,20-lyase and human placental aromatase enzymes. The structural features required for optimal inhibition o
Publikováno v:
Journal of Medicinal Chemistry. 38:2463-2471
Steroidal compounds having a 17-(3-pyridyl) substituent together with a 16,17-double bond have been synthesized, using a palladium-catalyzed cross-coupling reaction of a 17-enol triflate with diethyl(3-pyridyl)borane, which are potent inhibitors of h
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 50:267-273
Medical or surgical castration for the treatment of prostatic cancers prevents androgen production by the testes, but not by the adrenals. Inhibition of the key enzyme for androgen biosynthesis, cytochrome P450(17) alpha, could prevent androgen produ
Autor:
Martin G. Rowlands, S.E. Barrie, Raymond McCague, J. J. Deadman, John Houghton, Michael Jarman
Publikováno v:
Journal of Medicinal Chemistry. 33:2452-2455
In a search for inhibitors of 17 alpha-hydroxylase-C17,20-lyase and testosterone-5 alpha-reductase, target enzymes in the development of drugs to treat hormone-dependent prostatic cancer, we have identified certain compounds chemically derived by the
Publikováno v:
Journal of medicinal chemistry. 41(27)
Abiraterone (17-(3-pyridyl)androsta-5,16-dien-3beta-ol, 1) is a potent inhibitor (IC50 4 nM for hydroxylase) of human cytochrome P45017alpha. To assist in studies of the role of the 16,17-double bond in its mechanism of action, the novel 17alpha-(4-p
Autor:
Ben P. Haynes, Mitchell Dowsett, P.M. Goddard, Ferdinand Chan, Michael Jarman, Gerard A. Potter, S.E. Barrie
Publikováno v:
The Journal of steroid biochemistry and molecular biology. 60(5-6)
Two potent non-steroidal inhibitors (CB7645 and CB7661) of human cytochrome P450 17α were tested for in vivo activity in WHT mice. There were no signs of toxicity, but there was no effect on the androgen-dependent organs. The pharmacokinetics and bi
Publikováno v:
Journal of medicinal chemistry. 33(11)
A variety of esters of 4-pyridylacetic acid have been prepared by base mediated exchange from the methyl ester. Several of the esters of alcohols that contained a cyclohexyl ring were potent inhibitors of human placental aromatase and of the rat test
Publikováno v:
Journal of Steroid Biochemistry. 33:1191-1195
A simple assay for the measurement of the activities of both 17 alpha-hydroxylase and C17-C20 lyase is described. No extraction procedures are required. The separation of substrate and products is achieved using HPLC which allows the collection of th
Autor:
S.E. Barrie, Alan J. Williams
Publikováno v:
Biochemical and biophysical research communications. 84(1)
The relationship between the initial rates of respiration dependent calcium transport by isolated rabbit cardiac mitochondria and the free calcium concentration of the reaction media has been examined at 10°C and 25°C. Initial rates of calcium tran