Aromatase Inhibitors in Malignant Diseases of Aging

Johannessen, Dag Clement; Lønning, Per Eystein

doi:10.2165/00002512-199202060-00008

Cited by 12 publications

(1 citation statement)

References 123 publications

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“…Secondly, since the enzyme aromatase is involved in the final biosynthetic step, its inhibitors are of greater therapeutic interest) Further, inhibition of aromatase has been suggested to be important in the treatment of other malignant diseases in aging. 4 Recently researchers have provided a large body of evidence that supports the existence of a novel class of steroids which are devoid any known steroid hormone activity and have high specificity for the GABAA receptor complex (GRC), a iigand-gated chloride channel that mediates the inhibitory action of the neurotransmiter yaminobutyric acid (GABA). 5 These neuroactive steroids have been termed epalons, a shortened form of epiallopregnanolone, and putative epalon receptors may be unique sites on GRC that mediate the effects of neurosteroids on the GABA-gated channel function.…”

Section: Introductionmentioning

confidence: 99%

Improved syntheses of aromatase inhibitors and neuroactive steroids efficient oxidations and reductions at key positions for bioactivity

et al. 1999

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An Henbest reduction, followed by the preparation of a silyl enol ether and oxidation in situ with m-CPBA has led to the neurosteroids 3cz-hydroxy-and 3(x,21-dihydroxy-Scvpregnanolones. Using testosterone as starting material, a new short synthesis of an aromatase inhibitor, 4-OHA, has been achieved through hydroboration/oxidation followed by a Swem type oxidation and epimerization. Another aromatase inhibitor, androst-4-ene-3,6,17-trione, has been efficiently prepared using PCC on montmorillonite KI0, under ultrasonic irradiation.

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Section: Introductionmentioning

confidence: 99%

Improved syntheses of aromatase inhibitors and neuroactive steroids efficient oxidations and reductions at key positions for bioactivity

et al. 1999

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Dichlororuthenium(IV) Complex of meso‐Tetrakis(2,6‐dichlorophenyl)porphyrin: Active and Robust Catalyst for Highly Selective Oxidation of Arenes, Unsaturated Steroids, and Electron‐Deficient Alkenes by Using 2,6‐Dichloropyridine N‐Oxide

Zhang

Che

2005

Chemistry A European J

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[Ru(IV)(2,6-Cl2tpp)Cl2], prepared in 90 % yield from the reaction of [Ru(VI)(2,6-Cl2tpp)O2] with Me3SiCl and structurally characterized by X-ray crystallography, is markedly superior to [Ru(IV)(tmp)Cl2], [Ru(IV)(ttp)Cl2], and [Ru(II)(por)(CO)] (por=2,6-Cl2tpp, F20-tpp, F28-tpp) as a catalyst for alkene epoxidation with 2,6-Cl2pyNO (2,6-Cl2tpp=meso-tetrakis(2,6-dichlorophenyl)porphyrinato dianion; tmp=meso-tetramesitylporphyrinato dianion; ttp=meso-tetrakis(p-tolyl)porphyrinato dianion; F20-tpp=meso-tetrakis(pentafluorophenyl)porphyrinato dianion; F28-tpp=2,3,7,8,12,13,17,18-octafluoro-5,10,15,20-tetrakis(pentafluorophenyl)porphyrinato dianion). The "[Ru(IV)(2,6-Cl2tpp)Cl2]+2,6-Cl2pyNO" protocol oxidized, under acid-free conditions, a wide variety of hydrocarbons including 1) cycloalkenes, conjugated enynes, electron-deficient alkenes (to afford epoxides), 2) arenes (to afford quinones), and 3) Delta5-unsaturated steroids, Delta4-3-ketosteroids, and estratetraene derivatives (to afford epoxide/ketone derivatives of steroids) in up to 99 % product yield within several hours with up to 100 % substrate conversion and excellent regio- or diastereoselectivity. Catalyst [Ru(IV)(2,6-Cl2tpp)Cl2] is remarkably active and robust toward the above oxidation reactions, and turnover numbers of up to 6.4x10(3), 2.0x10(4), and 1.6x10(4) were obtained for the oxidation of alpha,beta-unsaturated ketones, arenes, and Delta5-unsaturated steroids, respectively.

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