DOCSLIB.ORG

See Phenacetin

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
See Phenacetin STP838-EB/May 1984 Index Bayer, G., 107 Barrall,E.M.,l A (see Anthracene) Beidellite, 134 Accuracy, 6, 13, 22-23, 31-38, 40, Benzamide, 52, 55-56, 59-60, 142 47-49,141-142 Benzene, 25, 90-105, 142 Acetone, 41 Bell Laboratories, 1 Acetonitrile, 25 Benzoic acid, 6-7 Acetophenetidin {see Phenacetin) Bias {see Accuracy) Activity, 92 Biotite, 131 Adiabatic calorimetry {see Calorime- Bismuth, 76-77 try, adiabatic) Blaine, Roger L., editor, 1, 17, 21, 29, Admixtures, 123 141 Alloys, 76-80, 86, 142 Boric anhyride, 76 Aluminum, 130, 133 Brennan, William, P., 2, 5, 21, Aluminum oxide, 76, 122, 125 141-142 American Cyanamid, 21 Brick clay {see Ceramic clay) American Society for Testing and Mate­ Bridge, Mueller, 96 rials, 1-2,16,19,21,24,29,31, 141, 143 Aminobenzoic acid {see Para-amino- benzoic acid) Calciostrontiaite series, 133 Ammonia, 76-77 Calcite, 124-125, 128-129 Ankerite, 130-131 Calcium, 128 Annealing, 76 Calcium carbonate, 125 Antimony, 76-77 Calorimetry, adiabatic, 90, 92-95, 97, Anthracene, 61, 63-70, 142 99-100,142 Aragonites, 130 Carbon dioxide, 123 Arsenates, 136 Carbonates, 122-124, 143 Arsenic, 76-77 Ceramic clay, 124-125, 143 Assay, 26 Cerussites, 130 ASTM {see American Society for Test­ Chalcocite, 128-129 ing and Materials) Chalcogenides, 136 Azeotrope, 96 Chlorites, 122, 134-135, 143 Azobenzene, 112-117, 119 Chloroform, 41 Cholestane, 42 Chromatography {see Gas chromatog­ B raphy. Liquid chromatography. Barium, 124, 130 Thin layer chromatography) 145 Copyright 1984 by AS FM International www.astm.org 146 INDEX Chromium, 82, 131, 135, 143 Dolomite, 123, 128-130 Circuitry, 96 Dopant, 52-53, 56 Clay {see Ceramic clay. Zeolites) Drugs {see Pharmaceuticals) Clinochlor, 135 Drying, 27 Colorimetry {see Spectrophotometry) DSC {see Differential scanning calo­ Composition, equivalent {see Equiva­ rimetry) lent composition) DTA {see Differential thermal analysis) Computer, 13, 23, 40, 108, 111 Du Pont Company {see E. I. du Pont de Concentration, 93 Nemours) Conductivity, electrical, 86 Dyes, 117 Copper, 78, 93, 128 Copper sulfide, 128-129 E Correction factor, 52 E. I. du Pont de Nemours, 1,17-21,24, Cryoscopy, 90-91, 96, 107, 142 31-30,40,42 Cryoscopic constant, 51, 59, 93, 99, BE {see Ethinyl estradiol) 107 ECG {see Equal G curve) Crystal defects, 122-123 Elder, J. P., 2, 21, 50, 142 Crystallization, 62,66-67,96-97,123, Electromotive force, 78-79, 81-82, 133 Curie temperature, 123, 131, 133 86-87, 142 Electron scattering {see Scattering, Current, % electron) D EMF {see Electromotive force) Data acquisition rate, 31, 35-36, 53 Encapsulation, 9-10 Decomposition, 123 Enthalpy of fusion, 7-8,30,49,51-52, Degradation 26, 31 56,65,68,92-93,99,107,113, Dehyroxylation, 123, 130, 133-134 118 Digenite, 128-129 Equal G curve, 67 Dibromobenzene, 66 Equivalent composition, 79-81 Dichlorobenzene, 66 Error, 6, 43, 48, 51, 81-82, 99 Differential Estrone, 41 Estrone methyl ether, 41 Scanning calorimetry, 5-15, 29, 39-40, 42-49, 50-51, 55, Ethinyl estradiol, 40-41, 43, 46-49 59-60, 61, 63, 65, 67-70, Ethinyl estradiol methy ether, 41 107-109, 112-115, 117-120, Eutectic,51,55,61-62,107-108,113, 141-143 132 Thermal analysis, 52, 121-136, 143 Dimethyl Formamide, 25 Fermi energy, 87-88 Sulfoxide, 25 Ferrillo, Rosalie G., 21 Dimethylnaphthalene, 61, 63-70, 142 Ferromagnetism, 131 Distribution coefficient, 61-62, 65 Ferrous {see Iron) DiVito, MichaelP.,5 Fisher Scientific Company, 18, 41 Djurleite, 128-129 Fraction melted {see Melt fraction) DMD {see Dimethylenaphthalene) Fraction, mole, 61, 65, 99, 107-108 INDEX 147 Fractional crystallization, 91, 142 Humidity, 23, 134 Freezing Hunter, John E.,m, 2, 29, 141 Curve, 91, 96 Hydroxides, 123, 143 Point, 62, 92 Hydrozincites, 130 Furukawa, George T., 2, 90, 142 Hygroscopicity, 27 Fyans, Richard L., 5 Hyperbolic function, 84 I Gallagher, P.K., 1 Ice, 76-77, 100 Gam, Paul, 21 IBM {see International Business Ma­ chines) Gas chromatography, 6, 27, 40, 42-46, 49, 63, 142 ICTA {see International Conference on Thermal Analysis) GC {see Gas chromatography) Geochemical laws, 132 Ideality, 104-105 Germanium, 76 Identity, 40 Gibbs-Duhem equation, 92 lUites, 134 Gill, Philip S., 21 Impurity level, 24, 32-35, 56, 82 Goethite, 130-131, 133 Impurities, 76, 80, 82, 107, 121-123, Gold, 95 141 Graphite, 76 Inclusions, 122 Indium, 49 Gray, A. P., 5-8, 10, 12-13, 15, 141 Guttman, Charles M., 1-2, 16, 21, 31, Infrared spectrophotometry, 27, 122 141 Institute of Crystallography and Gypsum, 124-125 Petrography, 107 Integration limits, 12 Interlaboratory tests, 17-20, 23 H International Business Machines, 1 International Conference on Thermal Heat capacity, 7, 11, 56, 93, 97-100 Analysis, 17, 24 Heat of fusion {see Enthalpy of fusion) International Practical Temperature Heater, 95-96 Scale, 81, 96 Heating rate, 7, 9-11, 23, 32-35, 42, International Union of Pure and Ap­ 48-49, 65, 110, 122 plied Chemistry, 91-92 Hectorite, 134 Iron, 82, 128-130, 133, 135 Helium, 100 Isomers, 112-113, 119 Heptane, 91, 96-97, 104-105, 142 Isomerization, 117 Hewlett Packard, 25, 40, 111 Isothermal Step Purity Method, 19-20, History, thermal, 12 25, 51, 55-58, 142 Hoffman-LaRochelnc, 1, 18, 20-21, lUPAC {see International Union of 24 Pure and Applied Chemistry) Homogeneity, 23, 26, 28 Hot stage microscopy {see Thermo- microscopy) HPLC {see Liquid chromatography) Jacobson, Harold, 21 148 INDEX K Temperature, 6-8, 51, 65-66, 70, Kalmmererites, 135-136 107-108, 113, 143 Kotschubeites, 135-136 Menis, O., 1, 21 Mestranol, 40, 43, 45, 47 Metals, 76,78, 80, 83-85, 88-89, 142 Methanol, 41-42 Lead, 76-77 Mettler Instruments Corporation, Lepidocrocite, 131 18-19, 63, 65, 107, 110, 122 Light, 23 Microcomputers (see Computers) Monochromatic, 112-113 Microscopy (see Thermomicroscopy) Polychromatic, 112-113 Mill, 25 Lim, Ofelia, 2, 39, 141 Minerals, 121-136, 142-143 Limits, integration (see Integration Mirabilite, 126 limits) Mixer, 25 Limonite, 131-132 MLR (see Multiple hnear regression) Linear regression (see Multiple linear Mole fraction (see Fraction, mole) regression) Molecular volume, 62 Liquid Monel, 94, 95 Chromatography, 25, 40, 42-43, 49 Monsanto Company, 21 Crystals, 112, 117 Montmorillonite, 134 Liquidus, 62, 65, 68 Moros, Stephen A., 1, 2, 18, 20-21, Lithium methoxide, 25 22, 141 MS (see Mass spectrometry) Multiple linear regression, 110-111 M Maghemite, 131 Magnesium, 128-129, 135 Magnesium oxide, 135 N Magnetic transition {see Curie tem­ National Bureau of Standards, 1, 16, perature) 21,25, 31,49,90-92,95-97 Magnetite, 131, 133 National Physical Laboratory, 112 Manganese, 82, 129, 131 NBS (see National Bureau of Stan­ Mass spectrometry, 27, 122, 126 dards) Materials, standard (see Standard ma­ NET (see Norethindrone) terials) Nickel, 81 Matthiessen's rule, 83 Nicolet Company, 25 Matrix, 24 Nitrogen, 41-42, 100 McGhie, Andrew R., 2, 61, 142 Nitric acid, 76 MEE (see Mestranol) NMR (see Nuclear magnetic reso­ Melt fraction, 8, 51, 58, 93, 102-103 nance) Melting Noise, 34, 36, 48 Curve, 7, 11, 23, 90-91 Nontronite, 134 Point (see Melting temperature) Norandrostendione, 41 Point depression, 7-8, 47-49, 50, Norethindrone, 41, 43-44, 47 107-108 Norethinyl testasterone, 41 INDEX 149 Norethynodrel, 41 Princeton Applied Research, 25 Norsethite, 124 Protocol, experimental, 17 Nuclear magnetic resonance, 25 PRS {see Standard materials) PRT {see Platinum resistance ther­ mometer) O Pump, 94, 95, 97 Oil, 76-78 Purity, 6, 23, 40, 75 Oliver, E., 39, 141 Pyrrhotite, 125, 121 Ortho Pharmaceutical, 39 Oxygen, 76 R Ramsland, Arnold, 25 Raoult's law, 91 Reference materials {see Standard ma­ Palermo, Eugene, 17 terials) Palygorskites, 134 Regression analysis {see Multiple lin­ PAMA (^see Para-aminobenzoic acid) ear regression) Para-aminobenzoic acid, 17, 24—28, Reilly, Martin L., 90 31, 52-57, 60, 141-142 Relative standard deviation {see Stan­ Partition coefficient, 59 dard deviation) Peak shape, 6-7 Resistance Pennwalt Corporation, 21 Electrical, 77-78, 80-81, 83, Perkin-Elmer Corporation, 5-6, 10, 85-87, 142 18-19, 21, 25, 40 Thermal, 9-11, 13, 83 Peritectic, 62, 68 Rhodochrosite, 131 Pharmaceuticals, 117 Riesen, R., 107 Pharmacopeia {see United States Phar­ Ripidolite, 135 macopeia) Round robin tests {see Interlaboratory Phase diagram, 61-67, 69, 122 tests) Phase solubility, 6, 19-20, 40 RSD {see Standard deviation) PHEN {see Phenacetin) Phenacetin, 17, 24-28, 31, 52-58, 60, 141 Phosphates, 136 Saponite, 134 Photomicrography, 28, 116, 119 Sapphire, 108, 112 Phyllosilicate, 134 Scanning rate {see Heating rate) Piccirelli, Jeanette H., 90 Scattering, electron, 87 Platinum, 122 Schaumann, Charles W., 21 Platinum resistance thermometer, 81, Scott, Charles E., 21 95-96, 142 Seals, vacuum, 95 Polarity, 83 Sepiolites, 134 Pollock, Daniel D., 2, 75, 142 Serpentines, 134 Potency, 40 Siderite, 130-131 Potential, electromotive, 96 Silicates, 135 Precision, 6, 13, 22, 35-37, 47-49, Silver, 76-77, 79, 82, 86, 142 141-142 Sintering, 123 150 INDEX Size Thermal lag {see Resistance, thermal) Particle, 27-28 Thermal resistance {see Resistance, Specimen, 9-10, 31-35, 42 thermal) Smectites, 12, 134 Thermocouple, 76, 78, 82-83, 86, 94, Smykatz-Kloss, Werner, 2, 121, 143 95, 110, 122 Sodium sulfate (see Thenardites) Thermoelectric effect, 76, 78 Solid solution, 28, 61-62, 64-67, 70, Thermogravimetry, 52, 122, 126 91, 92, 107, 122, 132, 142 Thermometer, platinum resistance Solidus, 62-63, 65-66, 69 {see Platinum resistance ther­ Solute, 62 mometer) Sondack correction method, 54-56, Thermomicroscopy, 63, 107-108, 113, 60, 110-111 116-117, 142-143 Specific heat {see Heat capacity)
Load more

Recommended publications
  • IJCB 42B(1) 166-172.Pdf
    Indian Journal of Chemistry Vol. 42B, January 2003, pp. 166-172 Synthesis and biological activity of 16-arylidene derivatives of estrone and estrone methyl ether Maninder Minu* & Dharam Paul lindal University In 5titutc of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India and G Leclercq & M Borras institut Jules Bordet, Association Hospitaliere de Bruxelles. Centre des Tumeurs de I'ULB, Rue Heger-Bordet 1- 1000, Belgiulll Received 24 April 200 I .. accepted (revised) 20 March 2002 The synthesis of 16-arylidene derivatives 3, 4, S, 6, 7. 8. 9, 10, 11, 12, 13, 14 and IS is described. These compounds have been tested at NCI, Bethesda, for their antineoplastic acti vity against the cell panel consisting of 60-ce!l lines and th e compounds 3, 4, S, 6 and 7 have also been tested for their ill vitro estrogenic / antiestrogenic activity; induction of ERE­ dependent luciferase inductio n was measured (MvLN celis). The formation of active steroids by aromatase has It was conceived that selective inhibitors of aroma­ been considered to play an important role in the de­ tase might be useful as a pharmacological tool to de­ velopment of human breast carcinoma t, at least one­ vice successful treatment approach for the hormonal third of all breast cancers establishing that. the estro­ dependent breast cancer. Our efforts were focused on gen-dependent carcinoma regresses following estro­ designing estrogen and estrogen methyl ether deriva­ 2 gen deprivation . In the postmenopausal women, the tives that might inhibit or possess antiestrogenic activ­ production of estrogen takes place in peripheral tissue ity. From these efforts, several 16-arylidine deriva­ 3 from inactive precursors by the action of aromatase .
    [Show full text]
  • Part I Biopharmaceuticals
    1 Part I Biopharmaceuticals Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 3 1 Analogs and Antagonists of Male Sex Hormones Robert W. Brueggemeier The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus, Ohio 43210, USA 1Introduction6 2 Historical 6 3 Endogenous Male Sex Hormones 7 3.1 Occurrence and Physiological Roles 7 3.2 Biosynthesis 8 3.3 Absorption and Distribution 12 3.4 Metabolism 13 3.4.1 Reductive Metabolism 14 3.4.2 Oxidative Metabolism 17 3.5 Mechanism of Action 19 4 Synthetic Androgens 24 4.1 Current Drugs on the Market 24 4.2 Therapeutic Uses and Bioassays 25 4.3 Structure–Activity Relationships for Steroidal Androgens 26 4.3.1 Early Modifications 26 4.3.2 Methylated Derivatives 26 4.3.3 Ester Derivatives 27 4.3.4 Halo Derivatives 27 4.3.5 Other Androgen Derivatives 28 4.3.6 Summary of Structure–Activity Relationships of Steroidal Androgens 28 4.4 Nonsteroidal Androgens, Selective Androgen Receptor Modulators (SARMs) 30 4.5 Absorption, Distribution, and Metabolism 31 4.6 Toxicities 32 Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 4 Analogs and Antagonists of Male Sex Hormones 5 Anabolic Agents 32 5.1 Current Drugs on the Market 32 5.2 Therapeutic Uses and Bioassays
    [Show full text]
  • EURL GUIDANCE on SUBSTANCES INCLUDED in the SUBSTANCE CATEGORIES LISTED in ANNEX I of SANTE 2017/11987
    DRAFT 24 September 2019 (EURLs ANSES, BVL and WFSR) EURL GUIDANCE ON SUBSTANCES INCLUDED IN THE SUBSTANCE CATEGORIES LISTED IN ANNEX I of SANTE 2017/11987 1. A1a Stilbenes (EURL WFSR Wageningen) Cfr. Substances listed for Group A1 in the MMPR Guidance 2. A1b Antithyroid agents (EURL WFSR Wageningen) Cfr. Substances listed for Group A2 in the MMPR Guidance 3. A1c Steroids (EURL WFSR Wageningen) Cfr. Substances listed for Group A3 in the MMPR Guidance 17b-Testosterone (4-Androsten-17b-ol-3-one) 17a-Testosterone (4-Androsten-17a-ol-3-one) 17a-Boldenone 17b-Boldenone Clostebol (CLTb) (4-androsten-4-chloro-17ß-ol-3-one) CLAD (4-chloro-4-androst-3,17-dione) (chloorandrosteendion) a-Estradiol (17a-Estradiol) 17b-estradiol (17ß-estradiol) Methylboldenone (1,4-Androstadien-17a-methyl-17b-ol-3-one) 17a-Methyltestosterone (4-Androsten-17a-methyl-17b-ol-3-one) 17b-Nortestosterone (b-nandrolone) 17α-Nortestosterone (4-estren-17a-ol-3-one) Ethinylestradiol (EE2) 17a-Trenbolone 17b-Trenbolone 16b-hydroxy-stanozolol Megestrol Melengestrol Chlormadinone Medroxyprogesterone Progesterone (P1) (4-Pregnene-3,20-dione (Pregnen(4)-3,20-dione)) Androsten-17ß-ol-3-one [1,(5a)-] (17b-1-testosteron) Mestranol (Ethynylestradiol 3-methyl ether) Fluoxymesterone (FMT) (4-androsten-9a-fluoro-17a-methyl-11ß,17ß-diol-3-one) DHEA (5-androsten-3b-ol-17-one) ethyl-5ß-estrane-3a,17ß-diol [17α-] (EED) Exemestane (6-Methyleneandrosta-1,4-diene-3,17-dione) Mesterolone (Androviron) Dromostanolone (Drostanolone) 2a-Methyl-5a-androstan-3a-ol-17-one
    [Show full text]
  • United States Patent Of?Ce 3,409,643 Patented Nov
    i United States Patent Of?ce 3,409,643 Patented Nov. 5, 1968 l 2 ’ 3,409,643 choire when preparing esters atI C-17 of l7a-alkynyl-l7? PROCESS FOR THE PREPARATION OF 1711 hydroxy steroids and particularly ' ALKYNL -l7?-ALKANOYLOXY STEROIDS of those steroids which OF THE ANDROSTANE AND ESTRANE also possess functions or systems ,(e.g. 3-methoxy-A2'5(1°> SERIES , and 3-ethoxy-A3,5.-) which are highly reactive or sensitive Elliot L. Shapiro, Cedar Grove, N.J., assignor to Schering Corporation, Bloom?eld, N.J., a corporation of New hydroxyl group. Thus, Jersey preparation of 3-methoxy-17a-ethinyl-2,5(10)-esteradien . No Drawing. Filed Mar. 11, 1966, Ser. No. 533,435 17,8-01 l7_-aeetate (an intermediate in the preparation of 10 Claims. (Cl. 260-—397.5) therapeutically valuable l9-n0r steroids) via methods 10 \ known in the art involves reacting 3-methoxy-l7a-ethinyl 2,5 ( 10)-estradien-17B-ol withv acetic anhydride in pyridine ' _ABSTRACT OF THE DISCLOSURE at elevated temperatures or with acetyl chloride in pyri A novel process for the preparation of 17a-alkynyl dine. Both the aforementioned reaction mediums cause l7?-alkanoyloxy steroids of the androstane and estrane ' involving destruction of the existing series comprises subjecting a 17~keto steroid of the andro A-ring sys em such as conversion of the 3-methoxy stane and estrane series to the ' ' Azimol- sys‘em to a 3-keto-l9-nor-A4- system or to an acetylide and adding in situ to the 17a-alkynyl-l7B-hy aromatic A-ring system (i.e.
    [Show full text]
  • Labeling and Synthesis of Estrogens and Their Metabolites
    Labeling and Synthesis of Estrogens and Their Metabolites Paula Kiuru University of Helsinki Faculty of Science Department of Chemistry Laboratory of Organic Chemistry P.O. Box 55, 00014 University of Helsinki, Finland ACADEMIC DISSERTATION To be presented with the permission of the Faculty of Science of the University of Helsinki, for public criticism in Auditorium A110 of the Department of Chemistry, A. I. Virtasen Aukio 1, Helsinki, on June 18th, 2005 at 12 o'clock noon Helsinki 2005 ISBN 952-91-8812-9 (paperback) ISBN 952-10-2507-7 (PDF) Helsinki 2005 Valopaino Oy. 1 ABSTRACT 3 ACKNOWLEDGMENTS 4 LIST OF ORIGINAL PUBLICATIONS 5 LIST OF ABBREVIATIONS 6 1. INTRODUCTION 7 1.1 Nomenclature of estrogens 8 1.2 Estrogen biosynthesis 10 1.3 Estrogen metabolism and cancer 10 1.3.1 Estrogen metabolism 11 1.3.2 Ratio of 2-hydroxylation and 16α-hydroxylation 12 1.3.3 4-Hydroxyestrogens and cancer 12 1.3.4 2-Methoxyestradiol 13 1.4 Structural and quantitative analysis of estrogens 13 1.4.1 Structural elucidation 13 1.4.2 Analytical techniques 15 1.4.2.1 GC/MS 16 1.4.2.2 LC/MS 17 1.4.2.3 Immunoassays 18 1.4.3 Deuterium labeled internal standards for GC/MS and LC/MS 19 1.4.4 Isotopic purity 20 1.5 Labeling of estrogens with isotopes of hydrogen 20 1.5.1 Deuterium-labeling 21 1.5.1.1 Mineral acid catalysts 21 1.5.1.2 CF3COOD as deuterating reagent 22 1.5.1.3 Base-catalyzed deuterations 24 1.5.1.4 Transition metal-catalyzed deuterations 25 1.5.1.5 Deuteration without catalyst 27 1.5.1.6 Halogen-deuterium exchange 27 1.5.1.7 Multistep labelings 28 1.5.1.8 Summary of deuterations 30 1.5.2 Enhancement of deuteration 30 1.5.2.1 Microwave irradiation 30 1.5.2.2 Ultrasound 31 1.5.3 Tritium labeling 32 1.6 Deuteration estrogen fatty acid esters 34 1.7 Synthesis of 2-methoxyestradiol 35 1.7.1 Halogenation 35 1.7.2 Nitration of estrogens 37 1.7.3 Formylation 38 1.7.4 Fries rearrangement 39 1.7.5 Other syntheses of 2-methoxyestradiol 39 1.7.6 Synthesis of 4-methoxyestrone 40 1.8 Synthesis of 2- and 4-hydroxyestrogens 41 2.
    [Show full text]
  • Biomarker Development to Assess Bone Health
    Copyright is owned by the Author of the thesis. Permission is given for a copy to be downloaded by an individual for the purpose of research and private study only. The thesis may not be reproduced elsewhere without the permission of the Author. Biomarker development to assess bone health A thesis presented in partial fulfilment of the requirements for the degree of Doctor of Philosophy in Nutritional Science at Massey University, Palmerston North, New Zealand. Diana Leticia Cabrera Amaro 2019 Abstract Postmenopausal women experience an accelerated bone loss with increased fracture risk caused by oestrogen deficiency. Biomarkers of bone turnover assess the changes of bone metabolism in postmenopausal women; however, prediction of bone loss with these common biomarkers cannot be achieved because bone biomarkers might not reflect the bone microenvironment status. Thus, there is a need for discovering new bone biomarkers that can efficiently predict bone loss in postmenopausal women. Previous studies suggest that the ovariectomised sheep in combination with injected glucocorticoids may be a reliable model to evaluate the biological response to oestrogen withdrawal as well as the bone remodelling process. The purpose of this research programme was to test the following hypotheses: 1) ovariectomising sheep in combination with monthly injections of glucocorticoids would result in decreased bone mineral density (BMD) and increased plasma bone remodelling marker concentration over a shorter period of time; 2) the plasma metabolome and lipidome of ovariectomised sheep would be different, and the biochemical changes in plasma and bone remodelling would be associated with bone loss; 3) and finally, there would also be a difference in the plasma metabolome and lipidome of Singaporean–Chinese postmenopausal women according to their bone mineral density status.
    [Show full text]
  • Biochem Press
    Internet Electronic Journal of Molecular Design 2003, 2, 435–453 ISSN 1538–6414 BioChem Press http://www.biochempress.com Internet Electronic Journal of Molecular Design July 2003, Volume 2, Number 7, Pages 435–453 Editor: Ovidiu Ivanciuc Special issue dedicated to Professor Nenad Trinajstiü on the occasion of the 65th birthday Part 1 Guest Editors: Douglas J. Klein and Sonja Nikoliü Using Simulated 2D 13C NMR Nearest Neighbor Connectivity Spectral Data Patterns to Model a Diverse Set of Estrogens Richard D. Beger, Kathleen J. Holm, Dan A. Buzatu, and Jon G. Wilkes Division of Chemistry, National Center for Toxicological Research, Food and Drug Administration, Jefferson, AR 72079 Received: March 21, 2003; Revised: May 2, 2003; Accepted: May 7, 2003; Published: July 31, 2003 Citation of the article: R. D. Beger, K. J. Holm, D. A. Buzatu, and J. G. Wilkes, Using Simulated 2D 13C NMR Nearest Neighbor Connectivity Spectral Data Patterns to Model a Diverse Set of Estrogens, Internet Electron. J. Mol. Des. 2003, 2, 435–453, http://www.biochempress.com. Copyright © 2003 BioChem Press R. D. Beger, K. J. Holm, D. A. Buzatu, and J. G. Wilkes Internet Electronic Journal of Molecular Design 2003, 2, 435–453 Internet Electronic Journal BioChem Press of Molecular Design http://www.biochempress.com Using Simulated 2D 13C NMR Nearest Neighbor Connectivity Spectral Data Patterns to Model a Diverse Set of Estrogens# Richard D. Beger,* Kathleen J. Holm, Dan A. Buzatu, and Jon G. Wilkes Division of Chemistry, National Center for Toxicological Research, Food and Drug Administration, Jefferson, AR 72079 Received: March 21, 2003; Revised: May 2, 2003; Accepted: May 7, 2003; Published: July 31, 2003 Internet Electron.
    [Show full text]
  • Structure-Activity Relationships for a Large Diverse Set of Natural, Synthetic, and Environmental Estrogens
    280 Chem. Res. Toxicol. 2001, 14, 280-294 Structure-Activity Relationships for a Large Diverse Set of Natural, Synthetic, and Environmental Estrogens Hong Fang,† Weida Tong,*,† Leming M. Shi,†,‡ Robert Blair,§ Roger Perkins,† William Branham,§ Bruce S. Hass,§ Qian Xie,† Stacy L. Dial,§ Carrie L. Moland,§ and Daniel M. Sheehan§ R.O.W. Sciences, Inc., 3900 NCTR Road, MC 910, Jefferson, Arkansas 72079, and Division of Genetic and Reproductive Toxicology, National Center for Toxicological Research, Jefferson, Arkansas 72079 Received October 3, 2000 Understanding structural requirements for a chemical to exhibit estrogen receptor (ER) binding has been important in various fields. This knowledge has been directly and indirectly applied to design drugs for human estrogen replacement therapy, and to identify estrogenic endocrine disruptors. This paper reports structure-activity relationships (SARs) based on a total of 230 chemicals, including both natural and xenoestrogens. Activities were generated using a validated ER competitive binding assay, which covers a 106-fold range. This study is focused on identification of structural commonalities among diverse ER ligands. It provides an overall picture of how xenoestrogens structurally resemble endogenous 17â-estradiol (E2) and the synthetic estrogen diethylstilbestrol (DES). On the basis of SAR analysis, five distinguishing criteria were found to be essential for xenoestrogen activity, using E2 as a template: (1) H-bonding ability of the phenolic ring mimicking the 3-OH, (2) H-bond donor mimicking the17â-OH and O-O distance between 3- and 17â-OH, (3) precise steric hydrophobic centers mimicking steric 7R- and 11â-substituents, (4) hydrophobicity, and (5) a ring structure. The 3-position H-bonding ability of phenols is a significant requirement for ER binding.
    [Show full text]
  • Steroids from Carvone Promotor Prof
    Steroids from Carvone Promotor Prof. dr. Ae. de Groot, Hoogleraar in de Bio-organische Chemie, Wageningen Universiteit Co-promotoren Prof. dr. M. B. Groen, Hoogleraar aan de Vrije Universiteit Amsterdam Dr. B. J. M. Jansen, Universitair Docent bij het Laboratorium voor Organische Chemie, Wageningen Universiteit Promotiecommissie Prof. dr. J. Wicha, Institute of Organic Chemistry, Polish Academy of Sciences, Warsaw, Poland Prof. dr. H. Hiemstra, Universiteit van Amsterdam Dr. J.W. Scheeren, Radboud Universiteit Nijmegen Prof. dr. E. J. R. Sudhölter, Wageningen Universiteit Florence C. E. Sarabèr Steroids from Carvone Proefschrift ter verkrijging van de graad van doctor op gezag van de rector magnificus van Wageningen Universiteit, Prof. dr. ir. L. Speelman, in het openbaar te verdedigen op dinsdag 10 mei 2005 des namiddags te half twee in de aula Sarabèr, Florence C. E. Steroids from Carvone Thesis Wageningen University –with references and summaries in English, French and Dutch ISBN 90-8504-181-3 Contents Chapter 1 1 Introduction Chapter 2 31 Domino Mukaiyama reactions to polycyclic systems Chapter 3 63 New approach towards C,D-trans fused steroid and D-homo steroid skeletons Chapter 4 85 A new and short synthesis of C,D-cis fused steroid and D-homosteroid skeletons Chapter 5 99 A second new and short synthesis of C,D-trans fused steroid skeletons Chapter 6 127 Synthesis of a chiral ring D precursor for the generation of enantiomerically pure steroid skeletons Chapter 7 145 1-Phenylthio-3-vinyl-3-cyclohexenol, a new reagent for bis-annelation of silyl enol ethers Chapter 8 165 The use of b-cyanoketones for the synthesis of functionalized polycyclic compounds Chapter 9 177 Discussion Appendix 187 List of used abbreviations 188 Summary 189 Samenvatting 195 Résumé 201 Dankwoord 207 Curriculum vitae 209 Wanneer jij je ogen opent zullen wij, opnieuw, op weg gaan tussen de uren en hun uitvindingen en slenterend tussen de verschijningen zullen wij de tijd en zijn vervoegingen bevestigen.
    [Show full text]
  • Pharmaceutical Compoundingand Dispensing, Second
    Pharmaceutical Compounding and Dispensing Pharmaceutical Compounding and Dispensing SECOND EDITION John F Marriott BSc, PhD, MRPharmS, FHEA Professor of Clinical Pharmacy Aston University School of Pharmacy, UK Keith A Wilson BSc, PhD, FRPharmS Head of School Aston University School of Pharmacy, UK Christopher A Langley BSc, PhD, MRPharmS, MRSC, FHEA Senior Lecturer in Pharmacy Practice Aston University School of Pharmacy, UK Dawn Belcher BPharm, MRPharmS, FHEA Teaching Fellow, Pharmacy Practice Aston University School of Pharmacy, UK Published by the Pharmaceutical Press 1 Lambeth High Street, London SE1 7JN, UK 1559 St Paul Avenue, Gurnee, IL 60031, USA Ó Pharmaceutical Press 2010 is a trade mark of Pharmaceutical Press Pharmaceutical Press is the publishing division of the Royal Pharmaceutical Society of Great Britain First edition published 2006 Second edition published 2010 Typeset by Thomson Digital, Noida, India Printed in Great Britain by TJ International, Padstow, Cornwall ISBN 978 0 85369 912 5 All rights reserved. No part of this publication may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, without the prior written permission of the copyright holder. The publisher makes no representation, express or implied, with regard to the accuracy of the information contained in this book and cannot accept any legal responsibility or liability for any errors or omissions that may be made. The right of John F Marriott, Keith A Wilson, Christopher A Langley and Dawn Belcher to be identified as the author of this work has been asserted by them in accordance with the Copyright, Designs and Patents Act, 1988.
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • G.P. Ellis (3).Pdf
    Progress in Medicinal Chemistry 16 This Page Intentionally Left Blank Progress in Medicinal Chemistry 16 Edited by G.P. ELLIS, D.SC., PH.D.,F.R.I.C. Department of Chemistry, University of Wales Institute of Science and Technology, King Edward VII Avenue, Card& CFl 3NU and G.B. WEST, B.PHARM., D.SC., PH.D., F.I.BIOL. Department of Paramedical Sciences, North East London Polytechnic, Romford Road, London El5 4LZ 1979 NORTH-HOLLAND PUBLISHING COMPANY AMSTERDAM.NEW YORK.OXFORD 0Elsevier/North-Holland Biomedical Press - 1979 AN rights reserved. No part of this publication may be reproduced, stored in a retrieval system. or transmitted in any form or by any means, electronic. mechanical, photocopying, recording or otherwise, without the prior permission of the copyright owner. ISBN for the series: 0 7204 7400 0 ISBN for this volume: 0 7204 0667 6 PUBLISHERS : Elsevier North-Holland Biomedical Press 335 Jan van Galenstraat, P.O. Box 21 1 Amsterdam, The Netherlands SOLE DISTRIBUTORS FOR THE U.S.A. AND CANADA: Elsevier/North-Holland Inc. 52 Vanderbilt Avenue New York, N.Y. 10017, U.S.A. LIBRARY OF CONGRESS CATALOGING IN PUBLICATION DATA Main entry under title: Progress in medicinal chemistry. London, Butterworths, 1961-1973 (Vols. 1-9). Amsterdam, North-Holland Publishing Co., 1974- (Vols. 10- ). Editors: 1961- G.P. Ellis and G.B. West. Includes bibliography. 1. Pharmacology-Collected works. 2. Chemistry, Medical and Pharmaceutical. I. Ellis, Gwynn Pennant, ed. 11. West, Geoffrey Buckle, 1961- ed. 111. Title: Medicinal chemistry. RS402.P78 615'.19 62-27 12 Photosetting by Thornson Press (India) Limited, New Delhi Printed in The Netherlands Preface We have pleasure in presenting five reviews in this volume.
    [Show full text]