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Synthesis and structure-activity relationships of 6-substituted androst-4-ene analogs as aromatase inhibitors.
Series of 6 alpha- and 6 beta-alkyl-substituted androst-4-en-17-ones (18 and 19) and their 17 beta-reduced derivatives (14 and 15)(alkyl: methyl, ethyl, n-propyl, n-pentyl, n-octyl) were synthesizedExpand
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Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.
A series of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their 7-deoxy derivatives, respectively, were synthesized and tested for their abilities to inhibit aromatase in human placentalExpand
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Time-dependent inactivation of aromatase by 6-alkylandrosta-1,4-diene-3,17-diones. Effects of length and configuration of 6-alkyl group.
Series of 6alpha- and 6beta-alkylandrosta-1,4-diene-3,17-diones (3 and 4) were synthesized and evaluated as time-dependent inactivators of aromatase in human placental microsomes to gain insights toExpand
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Mechanism for aromatase inactivation by a suicide substrate, androst-4-ene-3,6,17-trione. The 4 beta, 5 beta-epoxy-19-oxo derivative as a reactive electrophile irreversibly binding to the active site.
Aromatase is a cytochrome P450 enzyme complex that catalyzes the conversion of androst-4-ene-3,17-dione to estrone through three sequential oxygenations of the 19-methyl group.Expand
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4-Oxygenated androst-5-en-17-ones and their 7-oxo derivatives as aromatase inhibitors
A series of androst-5-ene-4,7-diones and 4-oxygenated androst-5-enes were synthesized and tested for their ability to inhibit aromatase in human placental microsomes. All of the steroids examinedExpand
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EPR studies of copper(II) and cobalt(II) complexes of adriamycin.
Cu2+ and Co2+ complexes of adriamycin (ADM) in aqueous solutions have been examined using EPR spectroscopy. An appreciable amount of Cu2+ and Co2+ complexes formed in the solutions were found to beExpand
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Studies directed toward a mechanistic evaluation of aromatase inhibition by androst-5-ene-7,17-dione: Time-dependent inactivation by the 19-nor and 5β,6β-epoxy derivatives
To gain further insight into the mechanism for inactivation of aromatase by androst-5-ene-7,17-dione (1) and its 19-nor analog 4, 10 beta-oxygenated steroids 5 and 6, delta 1(10)-steroid 7, andExpand
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A- or B-Ring-substituted derivatives of androst-4-ene-3,6,17-trione as aromatase inhibitors. Structure-activity relationships
2,2-Dimethylandrost-4-ene-3,6,17-trione (5) and its 4-methoxy- (7) and 4-hydroxy- (8) derivatives were synthesized. 7 alpha-Acetoxy-4-ene-3,6-dione steroid 2 was also prepared by the improved methodExpand
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Aromatization of 16α-hydroxyandrostenedione by human placental microsomes: effect of preincubation with suicide substrates of androstenedione aromatization
Estrogen synthase (aromatase) catalyzes the aromatization of androstenedione (AD) as well as 16alpha-hydroxyandrostenedione (16alpha-OHAD) leading to estrone and estriol, respectively. We found thatExpand
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