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1. Full Text Biological screening of cucurbitacin inspired estrone analogs targeting mitogen‐activated protein kinase (MAPK) pathway
by Ahmed, Mahmoud S and El‐Senduny, Fardous and Taylor, Jessica and Halaweish, Fathi T
Chemical Biology & Drug Design, ISSN 1747-0277, 09/2017, Volume 90, Issue 3, pp. 478 - 484
Assembly of cucurbitacin inspired estrone analogs has been previously synthesized and screened against melanoma cell lines. Further synthetic optimization was... 
estrone | MAPK pathway | Michael addition | melanoma | cucurbitacins | Estrone | Cucurbitacins | Melanoma | CELLS | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | ALPHA,BETA-UNSATURATED CARBONYL-COMPOUNDS | CANCER | Protein Structure, Tertiary | Cell Survival - drug effects | Cucurbitacins - chemistry | Phosphorylation | Mitogen-Activated Protein Kinase 3 - analysis | Enzyme-Linked Immunosorbent Assay | Humans | Cucurbitacins - metabolism | Mitogen-Activated Protein Kinase 1 - analysis | Estrone - toxicity | Estrone - analogs & derivatives | MAP Kinase Signaling System - drug effects | Mitogen-Activated Protein Kinase 3 - metabolism | Estrone - metabolism | Cell Line, Tumor | Molecular Docking Simulation | Cucurbitacins - toxicity | Binding Sites | Proto-Oncogene Proteins B-raf - metabolism | Mitogen-Activated Protein Kinase 1 - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Protein kinases | Mitogens | Index Medicus
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2. Full Text Docking, Synthesis, and in vitro Evaluation of Antimitotic Estrone Analogs
by Stander, Andre and Joubert, Fourie and Joubert, Annie
Chemical Biology & Drug Design, ISSN 1747-0277, 03/2011, Volume 77, Issue 3, pp. 173 - 181
In the present study, Autodock 4.0 was employed to discover potential carbonic anhydrase IX inhibitors that are able to interfere with microtubule dynamics by... 
virtual screening | mechanism‐based drug design | biological screening | Virtual screening | Mechanism-based drug design | Biological screening | CARBONIC-ANHYDRASE-IX | INHIBITS TUBULIN POLYMERIZATION | MULTITARGETED ANTITUMOR AGENTS | MICROTUBULES | BIOCHEMISTRY & MOLECULAR BIOLOGY | ENDOGENOUS MAMMALIAN METABOLITE | BREAST-CANCER CELLS | mechanism-based drug design | FORCE-FIELD | ANTICANCER DRUGS | 2-METHOXYESTRADIOL | CULTURES | Humans | Carbonic Anhydrase II - metabolism | Carbonic Anhydrases - chemistry | Estrone - therapeutic use | Antigens, Neoplasm - chemistry | Carbonic Anhydrase II - antagonists & inhibitors | Carbonic Anhydrase Inhibitors - toxicity | Carbonic Anhydrases - metabolism | Estrone - toxicity | Tubulin - metabolism | Cell Division | Computer Simulation | Drug Design | Antigens, Neoplasm - metabolism | G2 Phase | Female | Tubulin - chemistry | Binding Sites | Colchicine - chemistry | Carbonic Anhydrase IX | Carbonic Anhydrase Inhibitors - therapeutic use | Antimitotic Agents - toxicity | Antimitotic Agents - chemical synthesis | Carbonic Anhydrase Inhibitors - chemical synthesis | Breast Neoplasms - drug therapy | Antimitotic Agents - therapeutic use | Estrone - analogs & derivatives | Cell Line, Tumor | Software | Physiological aspects | Colchicine | Metastasis | Tubulins | Estradiol | Analysis | Index Medicus
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3. Full Text Design, synthesis, and biological evaluation of steroidal analogs as estrogenic/anti-estrogenic agents
by Alsayari, Abdulrhman and Kopel, Lucas and Ahmed, Mahmoud Salama and Pay, Adam and Carlson, Taylor and Halaweish, Fathi T
Steroids, ISSN 0039-128X, 02/2017, Volume 118, pp. 32 - 40
Series of estrone based analogs were synthetically investigated at positions C-9, C-11, C-16, and C-17 positions, to be biologically evaluated via assessment... 
Estrone | Breast cancer (MCF-7) cell lines | Breast cancer | Estrogenic/anti-estrogenic activity | BIOCHEMISTRY & MOLECULAR BIOLOGY | CELL-PROLIFERATION ASSAY | BREAST-CANCER THERAPY | MECHANISMS | ANTIESTROGENIC ACTIVITIES | MOLECULAR TARGETS | ENDOCRINOLOGY & METABOLISM | RECEPTOR MODULATORS | INHIBITORS | Receptors, Estrogen - metabolism | Estrogens - chemistry | Estrogens - pharmacology | Estrone - analogs & derivatives | MCF-7 Cells | Magnetic Resonance Spectroscopy | Humans | Female | Cell Proliferation - drug effects | Estrogens - chemical synthesis | Breast Neoplasms - metabolism | Drugstores | Analysis | Pharmacy | Estrogen | Index Medicus
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4. Full Text Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors
by Lawrence Woo, L.W and Leblond, Bertrand and Purohit, Atul and Potter, Barry V.L
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 04/2012, Volume 20, Issue 8, pp. 2506 - 2519
Estrone sulfamate (EMATE) is a potent irreversible inhibitor of steroid sulfatase (STS). In order to further expand SAR, the compound was substituted at the 2-... 
Endocrine therapy | EMATE | Breast cancer | Inhibitors | Steroid sulfatase | HUMAN-BREAST CANCER | CHEMISTRY, MEDICINAL | ESTRONE SULFATASE | ACTIVE-SITE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | 4-SUBSTITUTED ESTRONE | SITE-DIRECTED INHIBITION | RING | IN-VIVO ACTIVITIES | AROMATASE | DERIVATIVES | ESTROGENICITY | Estrone - pharmacology | Stereoisomerism | Humans | Enzyme Inhibitors - pharmacology | Structure-Activity Relationship | Enzyme Inhibitors - chemical synthesis | Estrone - chemical synthesis | Estrone - analogs & derivatives | Steryl-Sulfatase - antagonists & inhibitors | Estrone - chemistry | Enzyme Inhibitors - chemistry | Steryl-Sulfatase - metabolism | Molecular Structure | Heterocyclic compounds | Analysis | Index Medicus
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5. Full Text Synthesis of 2- and 17-substituted estrone analogs and their antiproliferative structure–activity relationships compared to 2-methoxyestradiol
by Shah, Jamshed H and Agoston, Gregory E and Suwandi, Lita and Hunsucker, Kimberly and Pribluda, Victor and Zhan, Xiaoguo H and Swartz, Glenn M and LaVallee, Theresa M and Treston, Anthony M
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 2009, Volume 17, Issue 20, pp. 7344 - 7352
A novel series of 17-modified and 2,17-modified analogs of 2-methoxyestradiol (2ME2) were synthesized and characterized. These analogs were designed to retain... 
Antiproliferative | 2-Methoxyestradiol analogs | Antiangiogenic | Structure–activity relationships | Structure-activity relationships | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | TUBULIN POLYMERIZATION | CHEMISTRY, ORGANIC | RECEPTOR | PROLIFERATION | INHIBITION | ANTIMITOTIC ACTIVITY | ESTRATROPONES | ESTRADIOL | CANCER-CELL-CULTURES | CYTOTOXICITY | METABOLITE | Cell Line | Estradiol - analogs & derivatives | Estrone - pharmacology | Animals | Estrone - chemistry | Humans | Rats | Cell Proliferation - drug effects | Structure-Activity Relationship | Estradiol - pharmacology | Estrone - chemical synthesis | Comparative analysis | Steroids | Index Medicus
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6. Full Text Synthesis of novel structurally simplified estrogen analogues
by Tietze, Lutz F and Vock, Carsten A and Krimmelbein, Ilga K and Wiegand, J Matthias and Nacke, Linda and Ramachandar, Tokala and Islam, Kazi M D and Gatz, Christiane
Chemistry (Weinheim an der Bergstrasse, Germany), ISSN 0947-6539, 2008, Volume 14, Issue 12, pp. 3670 - 3679
A library of 17 novel estrogen analogues 3 and 4 containing different substituents at rings A and D (steroid nomenclature) was prepared in a five- to... 
Vinyl halides | Palladium | Sonogashira reaction | Estrogens | Alkynes | Steroids | DOUBLE HECK REACTION | alkynes | estrogens | BETA MESSENGER-RNA | DL-ESTRONE | STEROID-HORMONES | CHEMISTRY, MULTIDISCIPLINARY | RECEPTOR-ALPHA | CORONARY-ARTERIES | PRELIMINARY COMMUNICATION | STEREOSELECTIVE SYNTHESIS | ALPHA ER-ALPHA | vinyl halides | palladium | steroids | CHANNELS | Estradiol - analogs & derivatives | Estradiol - chemistry | Estrone - analogs & derivatives | Estrone - chemistry | Stereoisomerism | Molecular Conformation | Small Molecule Libraries - chemical synthesis | Estradiol - chemical synthesis | Estrone - chemical synthesis | Index Medicus
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7. Full Text Glucosamine-6-sulfamate Analogues of Heparan Sulfate as Inhibitors of Endosulfatases
by Schelwies, Mathias and Brinson, Diana and Otsuki, Shuhei and Hong, Young-Hoon and Lotz, Martin K and Wong, Chi-Huey and Hanson, Sarah R
ChemBioChem, ISSN 1439-4227, 11/2010, Volume 11, Issue 17, pp. 2393 - 2397
Heparan sulfate | Sulfatases | Hydrolases | Inflammation | Inhibitors | inhibitors | CHEMISTRY, MEDICINAL | ESTRONE SULFATASE | MECHANISM | SULFOTRANSFERASES | BIOCHEMISTRY & MOLECULAR BIOLOGY | hydrolases | POTENT INHIBITORS | INACTIVATION | SYNTHETIC UTILITY | HEPATOCELLULAR-CARCINOMA | heparan sulfate | 6-O-ENDOSULFATASES | inflammation | BIOLOGICAL-ACTIVITY | sulfatases | STEROID SULFATASE | Sulfotransferases - genetics | Glucosamine - analogs & derivatives | Humans | Enzyme Inhibitors - pharmacology | Substrate Specificity | Glucosamine - chemistry | Hymecromone - metabolism | Arylsulfatases - metabolism | Dose-Response Relationship, Drug | Hymecromone - analogs & derivatives | Sulfotransferases - antagonists & inhibitors | Time Factors | Enzyme Inhibitors - chemistry | Heparitin Sulfate - analogs & derivatives | HEK293 Cells | Sulfotransferases - metabolism | Hymecromone - chemistry | Molecular Structure | Kinetics | Index Medicus
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8. Full Text Synthesis of aromatic stigmastanes: application to the synthesis of aromatic analogs of brassinosteroids
by Acebedo, Sofía L and Alonso, Fernando and Ramírez, Javier A and Galagovsky, Lydia R
Tetrahedron, ISSN 0040-4020, 05/2012, Volume 68, Issue 19, pp. 3685 - 3691
In this paper, we report the first synthesis of aromatic analogs of brassinosteroids. In order to accomplish this task, we explored two different synthetic... 
Brassinosteroids | Bioactivity | Aromatic stigmastanes | A-ring | PERCEPTION | STEROIDS | RECEPTOR KINASE BRI1 | 19-HYDROXY | CHEMISTRY, ORGANIC | ESTRONE | Sterols | Phytosterols | Steroids | Analogs | Synthesis (chemistry) | Tasks | Tetrahedrons | Biochemistry | Hormones | Brasses
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9. Full Text Absorption and metabolism of genistein and its five isoflavone analogs in the human intestinal Caco-2 model
by Chen, Jun and Lin, Huimin and Hu, Ming
Cancer Chemotherapy and Pharmacology, ISSN 0344-5704, 2/2005, Volume 55, Issue 2, pp. 159 - 169
The purposes of this study were to determine the effect of structural change on the intestinal disposition of isoflavones and to elucidate the mechanisms... 
Medicine | Metabolism | Isoflavone analogs | Caco-2 | Genistein | CELL-CULTURE MODEL | GLUCURONIDE | isoflavone analogs | FLAVONOIDS | DISPOSITION | MONOLAYERS | TRANSPORT | genistein | PHARMACOKINETICS | ONCOLOGY | DAIDZEIN | KINETICS | PHARMACOLOGY & PHARMACY | metabolism | PROTEIN-2 | Caco-2 Cells | Estrone - pharmacology | Absorption | Estrone - analogs & derivatives | Biological Transport | Genistein - metabolism | Humans | Isoflavones - metabolism | Leukotriene C4 - pharmacology | Index Medicus
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10. Full Text Synthesis of novel estrone analogs by incorporation of thiophenols via conjugate addition to an enone side chain
by Kopel, Lucas C and Ahmed, Mahmoud S and Halaweish, Fathi T
Steroids, ISSN 0039-128X, 11/2013, Volume 78, Issue 11, pp. 1119 - 1125
Functionalized estrogen analogs have received interest due to their unique and differing biological activity compared to their parent compounds. The synthesis... 
Aldol | Sulfa-Michael addition | Estrone | Thiol | Enone | ALPHA,BETA-UNSATURATED KETONES | ANTICANCER AGENTS | BIOCHEMISTRY & MOLECULAR BIOLOGY | TUBULIN POLYMERIZATION | CARBONYL-COMPOUNDS | ANTITUMOR-ACTIVITY | ESTROGENIC ACTIVITY | BREAST-CANCER | IN-VITRO | ENDOCRINOLOGY & METABOLISM | STEREOSELECTIVE-SYNTHESIS | Alkenes - chemistry | Chemistry Techniques, Synthetic | Estrone - analogs & derivatives | Estrone - chemistry | Molecular Conformation | Ketones - chemistry | Models, Molecular | Phenols - chemistry | Sulfhydryl Compounds - chemistry | Estrone - chemical synthesis | Incorporation | Index Medicus
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11. Full Text Synthesis and Anti-Angiogenic Activity of Cortistatin Analogs
by SATO, Yuuki and KAMIYAMA, Hiroshi and USUI, Takeo and SAITO, Tamio and OSADA, Hiroyuki and KUWAHARA, Shigefumi and KIYOTA, Hiromasa
Bioscience, Biotechnology, and Biochemistry, ISSN 0916-8451, 11/2008, Volume 72, Issue 11, pp. 2992 - 2997
Analogs of cortistatins, a series of anti-angiogenic compounds isolated from the Indonesian marine sponge Cortisium simplex, were synthesized from estrone by... 
synthesis | HUVEC | cortistatin A | angiogenesis | Cortisium simplex | Cortistatin A | Angiogenesis | Synthesis | STEROIDAL ALKALOIDS | BIOTECHNOLOGY & APPLIED MICROBIOLOGY | SPONGE CORTICIUM-SIMPLEX | BIOCHEMISTRY & MOLECULAR BIOLOGY | FOOD SCIENCE & TECHNOLOGY | CHEMISTRY, APPLIED | Cell Line | Humans | Angiogenesis Inhibitors - pharmacology | Cell Movement - drug effects | Animals | Estrone - analogs & derivatives | Endothelial Cells - cytology | Neuropeptides - pharmacology | Cell Proliferation - drug effects | Mice | Neuropeptides - chemical synthesis | Vascular Endothelial Growth Factor A - pharmacology | Angiogenesis Inhibitors - chemical synthesis | Angiogenesis Inhibitors - chemistry | Endothelial Cells - drug effects | Neuropeptides - chemistry | Index Medicus
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12. Preparation of five estrone analogs and theoretical analysis of its interaction with aromatase enzyme
by Rosas-Nexticapa, Marcela and Figueroa-Valverde, Lauro and Cedillo, Francisco Diaz and Camacho-Luis, Abelardo and Mateu-Armand, Virginia and Herrera-Meza, Socorro and García-Cervera, Elodia and Gómez, Eduardo Pool and Lopez-Ramos, Maria and Hau-Heredia, Lenin and Estrella-Barron, Raquel and Alfonso-Jimenez, Alondra and Cabrera-Tuz, Jhair and Noh-Delgado, Raquel and Mari-Parra, Alexandrea
Biointerface Research in Applied Chemistry, 12/2018, Volume 8, Issue 6, pp. 3644 - 3651
Estrone derivatives | Aromatase | Docking | Breast cancer
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13. Full Text Synthesis of ferrocenestrone: The first metallocene based steroid analogue
by Hessler, Filip and Císařová, Ivana and Sedlák, David and Bartůněk, Petr and Kotora, Martin
Chemistry - A European Journal, ISSN 0947-6539, 04/2012, Volume 18, Issue 18, pp. 5515 - 5518
Ferrocenestrone, the first steroid derivative containing a metallocene moiety, was stereoselectively prepared. The key steps included the enantioselective... 
ferrocenestrones | steroids | asymmetric synthesis | synthesis design | metallocenes | (+)-ESTRONE | HYDROGENATION | FORMAL TOTAL-SYNTHESIS | RECEPTOR | ESTRONE | CHEMISTRY, MULTIDISCIPLINARY | SKELETON | BOND FORMATION REACTION | CHEMISTRY | CHIRALITY | DERIVATIVES | Chemistry Techniques, Synthetic | Organometallic Compounds - chemical synthesis | Stereoisomerism | Ferrous Compounds - chemical synthesis | Models, Molecular | Crystallography, X-Ray | Organometallic Compounds - chemistry | Ferrous Compounds - chemistry | Metallocenes | Hydrogenation | Steroids - chemical synthesis | Steroids - chemistry | Index Medicus | Diels-Alder reactions | Inversions | Derivatives | Bonding | Elongation | Steroids
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14. Full Text Synthesis and some biological properties of sulfamates derived from 8α-analogs of steroidal estrogens
by Morozkina, S N and Gluzdikov, I A and Drozdov, A S and Selivanov, S I and Kovalev, R A and Filatov, M V and Shavva, A G
Russian Journal of Organic Chemistry, ISSN 1070-4280, 3/2015, Volume 51, Issue 3, pp. 411 - 416
Sulfamates derived from estrogens of the 8α-series have been synthesized, and their effect on the growth of MCF-7 breast cancer cells has been studied. The... 
Chemistry | Organic Chemistry | BREAST-CANCER | 17-BETA-HYDROXYSTEROID-DEHYDROGENASE TYPE-1 | THERAPY | ESTRONE SULFATASE | ANALOGS | ESTRADIOL | CHEMISTRY, ORGANIC | RECEPTOR MODULATORS | POTENT INHIBITORS | DERIVATIVES | SULFATASE INHIBITORS
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15. Full Text Neuroprotective effects of a novel non-receptor-binding estrogen analogue: In vitro and in vivo analysis
by Liu, Ran and Yang, Shao-Hua and Perez, Evelyn and Yi, Kun Don and Wu, Samuel S and Eberst, Kathleen and Prokai, Laszlo and Prokai-Tatrai, Katalin and Cai, Zu Yun and Covey, Douglas F and Day, Arthur L and Simpkins, James W
Stroke, ISSN 0039-2499, 10/2002, Volume 33, Issue 10, pp. 2485 - 2491
Background and Purpose-Although estrogens are neuroprotective, hormonal effects limit their clinical application. Estrogen analogues with neuroprotective... 
Neuroprotection | Receptors, estrogen | Ischemia | Cerebral blood flow | Estrogens | Reperfusion injury | MORTALITY | OXIDATIVE STRESS | MONICA PROJECT | ACTIVATED PROTEIN-KINASE | estrogens | RISK | reperfusion injury | EXPERIMENTAL STROKE | POSTMENOPAUSAL HORMONE-THERAPY | 17-BETA-ESTRADIOL | CLINICAL NEUROLOGY | ischemia | ISCHEMIC DAMAGE | neuroprotection | receptors, estrogen | ESTRADIOL | cerebral blood flow | PERIPHERAL VASCULAR DISEASE | Estradiol - analogs & derivatives | Receptors, Estrogen - metabolism | Humans | Neurons - cytology | Estradiol Congeners - chemistry | Drug Carriers | Dose-Response Relationship, Drug | Brain - blood supply | Estrogen Receptor alpha | Neuroprotective Agents - pharmacology | Female | Infarction, Middle Cerebral Artery - drug therapy | Neurons - drug effects | Estradiol - pharmacology | Adamantane - analogs & derivatives | Disease Models, Animal | Cell Line | Cell Survival - drug effects | Adamantane - pharmacology | Estrone - pharmacology | Neuroprotective Agents - chemistry | Cerebrovascular Circulation - drug effects | Estradiol Congeners - pharmacology | Rats | Infarction, Middle Cerebral Artery - pathology | Rats, Sprague-Dawley | Binding, Competitive - drug effects | Brain - drug effects | Estradiol - chemistry | Animals | Estrone - analogs & derivatives | Receptors, Estrogen - chemistry | Estrone - chemistry | Brain - pathology | Ligands | Mice | Adamantane - chemistry | Glutamic Acid - toxicity | Estrogen Receptor beta | Blood Flow Velocity - drug effects | Index Medicus
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16. Full Text Synthesis of BCD tricyclic analogues of the novel cardiac glycoside rhodexin A
by Jung, Michael E and Chu, Hiufung V
Tetrahedron Letters, ISSN 0040-4039, 2011, Volume 52, Issue 35, pp. 4512 - 4514
A concise synthesis of the two BCD tricyclic analogues and of the cardiac glycoside rhodexin A is described. A concise synthesis of novel cardiac glycoside... 
Glycoside synthesis | Terpene synthesis | Diels–Alder reaction | Inverse-electron-demand | Diels-Alder reaction | JAPONICA | VON OUABAGENIN | (+/-)-ESTRONE | (+/-)-ADRENOSTERONE | CHEMISTRY, ORGANIC | DIGITALIS | DIGITOXIN | OUABAIN | STEREOSELECTIVE TOTAL SYNTHESIS | SYSTEMS | GLYKOSIDE UND AGLYKONE | Heterocyclic compounds | Demand | Diels-Alder reactions | Synthesis (chemistry) | Construction | Tetrahedrons | Glycosides | Ethers
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17. Full Text Steroids and steroid analogues from Stille-Heck coupling sequences
by Sünnemann, Hans Wolf and De Meijere, Armin
Angewandte Chemie - International Edition, ISSN 1433-7851, 02/2004, Volume 43, Issue 7, pp. 895 - 897
Cross-coupling | Pericyclic reactions | Homogeneous catalysis | Total synthesis | Steroids | pericyclic reactions | homogeneous catalysis | PALLADACYCLES | cross-coupling | steroids | total synthesis | DL-ESTRONE | RING OPENINGS | EFFICIENT | CHEMISTRY, MULTIDISCIPLINARY | CATALYSTS | COBALT | Chemistry, Organic - methods | Naphthalenes - chemistry | Alkenes - chemistry | Polycyclic Compounds - chemistry | Cyclization | Stereoisomerism | Molecular Structure | Catalysis | Steroids - chemical synthesis | Index Medicus
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18. Full Text A facile total synthesis of ent-17β-estradiol and structurally related analogues
by Cai, Zu Yun and Covey, Douglas F
Steroids, ISSN 0039-128X, 2007, Volume 72, Issue 4, pp. 351 - 359
A facile six-step synthesis (15.2% yield) of -17β-estradiol from readily accessible precursors is described. The preparation of analogues with 2-alkyl... 
Antioxidants | Estradiol analogues | Neuroprotectants | Enantiomer | Ent-17β-estradiol | ESTROGENS | ent-17 beta-estradiol | OXIDATIVE STRESS | TOTAL ANTIOXIDATIVE ACTIVITIES | ENANTIOSELECTIVE SYNTHESIS | antioxidants | BIOCHEMISTRY & MOLECULAR BIOLOGY | neuroprotectants | estradiol analogues | STEROID-HORMONES | ESTRONE | CYCLOADDITION | IN-VITRO | ESTRADIOL | ENDOCRINOLOGY & METABOLISM | enantiomer | BIOLOGICAL EVALUATION | ent-17β-estradiol
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