M
Michael Jarman
Researcher at Brunel University London
Publications - 119
Citations - 4343
Michael Jarman is an academic researcher from Brunel University London. The author has contributed to research in topics: Metabolite & Idoxifene. The author has an hindex of 33, co-authored 119 publications receiving 4251 citations.
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Journal ArticleDOI
Hormonal impact of the 17 alpha-hydroxylase/C-17,C-20-lyase inhibitor abiraterone acetate (CB7630) in patients with prostate cancer
A. O'Donnell,Ian Judson,Mitch Dowsett,Florence I. Raynaud,David P. Dearnaley,Malcolm David Mason,S. Harland,A. Robbins,Gavin Halbert,Bernard Nutley,Michael Jarman +10 more
TL;DR: Repeated treatment of men with intact gonadal function with abiraterone acetate at a dose of 800 mg can successfully suppress testosterone levels to the castrate range, however, this level of suppression may not be sustained in all patients due to compensatory hypersecretion of LH.
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Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer.
TL;DR: 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- pyridol)borane, which are potent inhibitors of human testicular 17 alpha-hydroxylase-C17,20-lyase.
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Some studies of the active intermediates formed in the microsomal metabolism of cyclophosphamide and isophosphamide.
TL;DR: It appeared that, of the known metabolites of cyclophosphamide, only phosphoramide mustard possesses the cytoxicity and biological half-life appropriate to the active antitumour metabolite, and four other metabolites of low cytotoxicity were isolated and identified.
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Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity.
Lindsay Stimson,Martin G. Rowlands,Yvette Newbatt,Nicola F. Smith,Florence I. Raynaud,Paul Rogers,Vassilios Bavetsias,Stephen Gorsuch,Michael Jarman,Andrew J. Bannister,Tony Kouzarides,Edward McDonald,Paul Workman,G. Wynne Aherne +13 more
TL;DR: A series of isothiazolone-based HAT inhibitors were identified and chemical reactivity of these compounds, as measured by covalent protein binding and loss of HAT inhibition in the presence of DTT, indicated that reaction with thiol groups might be important in their mechanism of action.
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A new cytotoxic, DNA interstrand crosslinking agent, 5-(aziridin-1-yl)-4-hydroxylamino-2-nitrobenzamide, is formed from 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by a nitroreductase enzyme in Walker carcinoma cells.
TL;DR: A new compound can form interstrand crosslinks in the DNA of Chinese hamster V79 cells to which it is also highly toxic, findings indicative of the formation by Walker cells of a diffusible toxic metabolite of CB 1954.