212 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Analogue based drug design, synthesis, molecular docking and anticancer evaluation of novel chromene sulfonamide hybrids as aromatase inhibitors and apoptosis enhancers.
King Saud University
Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.
Temple University School of Pharmacy
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptorsa andß.
Purdue University
Recent developments of C-4 substituted coumarin derivatives as anticancer agents.
Central University of Punjab
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.
State University of New York Upstate Medical University
Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors.
University of Chieti 'G. d'Annunzio'
Exploring new chemical functionalities to improve aromatase inhibition of steroids.
University of Coimbra
Isocoumarins, miraculous natural products blessed with diverse pharmacological activities.
Quaid-i-Azam University
Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid Biosynthesis.
University of Bologna
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.
The M. S. University of Baroda
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.
American University of Ras Al Khaimah
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.
University of Bath
Synthesis and molecular docking of 1,2,3-triazole-based sulfonamides as aromatase inhibitors.
Srinakharinwirot University
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11ß-Hydroxylase.
Saarland University
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.
Purdue University
Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.
Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
Exemestane metabolites: Synthesis, stereochemical elucidation, biochemical activity and anti-proliferative effects in a hormone-dependent breast cancer cell line.
University of Coimbra
Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.
Saarland University
Bioactive benzofuran derivatives: moracins A-Z in medicinal chemistry.
Dongguk University-Seoul
Spongiapyridine and related spongians isolated from an Indonesian Spongia sp.
University of Hawaii at Manoa
Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
Discovery of new 7-substituted-4-imidazolylmethyl coumarins and 4'-substituted-2-imidazolyl acetophenones open analogues as potent and selective inhibitors of steroid-11ß-hydroxylase.
Universit£ degli Studi di Bari"Aldo Moro"
Discovery of a new class of cinnamyl-triazole as potent and selective inhibitors of aromatase (cytochrome P450 19A1).
McMaster University
Inhibitory effect of Rhus verniciflua Stokes extract on human aromatase activity; butin is its major bioactive component.
Hanyang University
Investigation of fluorinated and bifunctionalized 3-phenylchroman-4-one (isoflavanone) aromatase inhibitors.
Northern Kentucky University
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Novartis Institutes for BioMedical Research
Investigation of aryl halides as ketone bioisosteres: refinement of potent and selective inhibitors of human cytochrome P450 19A1 (aromatase).
McMaster University
Design, synthesis, and structure-activity relationships of azolylmethylpyrroloquinolines as nonsteroidal aromatase inhibitors.
University of Padova
Chemopreventive and antioxidant activity of 6-substituted imidazo[2,1-b]thiazoles.
Universit£ di Bologna
Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.
Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.
Purdue University
Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives.
Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University)
Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11ß-hydroxylase inhibition.
University of Bologna
Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.
Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
Institute of Cancer Research
Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
TBA
Optimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1).
Purdue University
Novel aromatase inhibitors by structure-guided design.
State University of New York Upstate Medical University
Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.
Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome.
Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
New structure-activity relationships of A- and D-ring modified steroidal aromatase inhibitors: design, synthesis, and biochemical evaluation.
University of Coimbra
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.
Northern Kentucky University
Radical scavenging and antioxidant activities of isocoumarins and a phthalide from the endophytic fungus Colletotrichum sp.
Chulabhorn Institute
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.
Saarland University
Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer.
Purdue University
Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation.
University of Bologna
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Johns Hopkins University
Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
University of Bath
Screening of herbal constituents for aromatase inhibitory activity.
King's College London
Selective inhibition of aromatase by a dihydroisocoumarin from Xyris pterygoblephara.
Universidade Federal de Minas Gerais
"Virtual fragment linking": an approach to identify potent binders from low affinity fragment hits.
Novartis Institutes for BioMedical Research
New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
UPRES EA 4021 Biomol�cules et Th�rapies anti-tumorales
Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: synthesis, biological evaluation, and ligand-based pharmacophore identification.
The Ohio State University
Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
Purdue University
Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.
University of Oporto
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of a new series of mechanism-based aromatase inhibitors.
Centre de Recherches Roussel-Uclaf
Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors.
Tohoku College of Pharmacy
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
Ciba-Geigy Corporation
Mechanism and inhibition of cytochrome P-450 aromatase.
Johns Hopkins University School of Medicine
Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione.
Washington University
Interactions of thiol-containing androgens with human placental aromatase.
University of Washington
Analogues of aminoglutethimide: selective inhibition of cholesterol side-chain cleavage.
TBA
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.
Purdue University
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.
Novartis Institutes for BioMedical Research
Optimizing thiadiazole analogues of resveratrol versus three chemopreventive targets.
Purdue University
Discovery of a novel class of aldol-derived 1,2,3-triazoles: potent and selective inhibitors of human cytochrome P450 19A1 (aromatase).
McMaster University
Design, synthesis, and biological evaluation of callophycin A and analogues as potential chemopreventive and anticancer agents.
University of Hawaii at Hilo
Recent progress in synthesis and bioactivity studies of indolizines.
University of Botswana
Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors.
Universit£ de Moncton
Structure-based design of potent aromatase inhibitors by high-throughput docking.
Universita` di Modena e Reggio Emilia
Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.
UPRES EA 4021 Biomol�cules et Th�rapies anti-tumorales
Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.
Saarland University
Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-a-hydroxylase/C17-20 lyase.
Universita` degli Studi di Bari Aldo Moro
Hybrid Dual Aromatase-Steroid Sulfatase Inhibitors with Exquisite Picomolar Inhibitory Activity
TBA
N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).
Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland
Molecular docking and QSAR study on steroidal compounds as aromatase inhibitors.
Tianjin University of Science and Technology
Exploring benzcyclo derivatives as potent aromatase inhibitors using ligand-based modeling studies.
University of Calcutta
Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Saarland University
Aspergillusol A, an alpha-glucosidase inhibitor from the marine-derived fungus Aspergillus aculeatus.
Institute and the Center for Environmental Health
An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
Universidade de Coimbra
Monodictyochromes A and B, Dimeric Xanthone Derivatives from the Marine Algicolous Fungus Monodictys putredinis.
University of Bonn
Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)).
University of the West of Scotland
Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Universidade de Coimbra
In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Saarland University
CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.
Università di Salerno
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.
Saarland University
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.
Saarland University
Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.
Université de Nantes
Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity.
University of Illinois at Chicago
Evaluation of ursolic acid isolated from Ilex paraguariensis and derivatives on aromatase inhibition.
Universidade Federal do Rio Grande do Sul (UFRGS)
Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.
University of Illinois at Chicago
Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells.
The Ohio State University
Potential cancer chemopreventive in vitro activities of monomeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.
University of Bonn
Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
University of Bologna
Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.
The Ohio State University
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors.
Nantes University
Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
UPRES EA 1085 Biomolécules et Cibles Cellulaires Tumorales
Balanced dual acting compounds targeting aromatase and estrogen receptor ? as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.
Alma Mater Studiorum-University of Bologna
Diterpenoids with Aromatase Inhibitory Activity from the Rhizomes of
Chulabhorn Royal Academy
Synthesis, structure-activity relationships and molecular docking studies of phenyldiazenyl sulfonamides as aromatase inhibitors.
"G. d'Annunzio" University
Design, synthesis and biological evaluation of imidazole and triazole-based carbamates as novel aromatase inhibitors.
"G. D'Annunzio" University
Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
Bristol-Myers Squibb Pharmaceutical Research Institute
Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.
UFR des Sciences Pharmaceutiques
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.
Purdue University
Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.
UPRES EA 1085
New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.
UPRES EA 1085
A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.
University of Bologna
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors.
Alma Mater Studiorum-University of Bologna
Synthesis and evaluation of 17-aliphatic heterocycle-substituted steroidal inhibitors of 17alpha-hydroxylase/C17-20-lyase (P450 17).
University of the Saarland
Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.
Key Laboratory of Industrial Fermentation Microbiology (Tianjin University of Science & Technology)
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
University of Washington
Sulfamates in drug design and discovery: Pre-clinical and clinical investigations.
University of Sharjah
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.
Indian Institute of Technology (BHU)
1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.
Cardiff University
C-6?- vs C-7?-Substituted Steroidal Aromatase Inhibitors: Which Is Better? Synthesis, Biochemical Evaluation, Docking Studies, and Structure-Activity Relationships.
University of Coimbra
Rational design of allosteric modulators of the aromatase enzyme: An unprecedented therapeutic strategy to fight breast cancer.
CNR-IOM-Democritos c/o International School for Advanced Studies (SISSA)
New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles.
Nantes
Synthesis, molecular docking, and QSAR study of bis-sulfonamide derivatives as potential aromatase inhibitors.
Srinakharinwirot University
Design and synthesis of a new type of non steroidal human aromatase inhibitors.
Centre d'Etudes et de Recherche sur le Médicament de Normandie
Indole: A privileged scaffold for the design of anti-cancer agents.
Hunan University of Science and Technology
Synthesis of ?-methylstilbenes using an aqueous Wittig methodology and application toward the development of potent human aromatase inhibitors.
McMaster University
6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
University of Minnesota
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
SmithKline Beecham Pharmaceuticals Ltd
Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors.
"G. d'Annunzio" University
3- and 4-pyridylalkyl adamantanecarboxylates: inhibitors of human cytochrome P450(17 alpha) (17 alpha-hydroxylase/C17,20-lyase). Potential nonsteroidal agents for the treatment of prostatic cancer.
Cancer Research Campaign Centre for Cancer Therapeutics
Development of Highly Selective Pyrimidine-Based Aldosterone Synthase (CYP11B2) Inhibitors.
Selenity Therapeutics
Tetrahydronaphthalenes: influence of heterocyclic substituents on inhibition of steroid enzymes P450 arom and P450 17.
Universität de Saarlandes
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Novartis Institutes for BioMedical Research
Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.
Ciba-Geigy Ltd
Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.
Syntex Discovery Research
6-Alkyl- and 6-arylandrost-4-ene-3,17-diones as aromatase inhibitors. Synthesis and structure-activity relationships.
Tohoku College of Pharmacy
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
Universität des Saarlandes
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.
Tohoku College of Pharmacy
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
Universität des Saarlandes
Synthesis, structure elucidation, and biochemical evaluation of 7 alpha- and 7 beta-arylaliphatic-substituted androst-4-ene-3,17-diones as inhibitors of aromatase.
Ohio State University
Novel steroidal inhibitors of human cytochrome P45017 alpha (17 alpha-hydroxylase-C17,20-lyase): potential agents for the treatment of prostatic cancer.
Institute of Cancer Research
Probing the hydrophobic pocket of the active site of aromatase with 4-phenoxy-7 alpha-(phenylthio)-4-androstene-3,17-dione.
University of Minnesota
Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis.
CRC Laboratory
Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
TBA
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
TBA
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
TBA
Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives.
Istanbul Medipol University
Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
Boehringer Ingelheim Pharmaceuticals
Structure-activity relationships and docking studies of synthetic 2-arylindole derivatives determined with aromatase and quinone reductase 1.
University of Hawai'i at Hilo
Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17?-Hydroxysteroid Dehydrogenase Type 2.
University of Basel
Potent aromatase inhibitors and molecular mechanism of inhibitory action.
Yunnan University
Synthesis, molecular docking, and QSAR study of sulfonamide-based indoles as aromatase inhibitors.
Srinakharinwirot University
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analogue, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives.
Institute of Cancer Research
Synthesis and biochemical studies of 7-substituted 4,6-androstadiene-3,17-diones as aromatase inhibitors.
Ohio State University
Inhibition of enzymes of estrogen and androgen biosynthesis by esters of 4-pyridylacetic acid.
Institute of Cancer Research
Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17?-hydroxylase-C17,20-lyase (Cyp17).
Temple University School of Pharmacy
Design and optimization of highly-selective, broad spectrum fungal CYP51 inhibitors.
Viamet Pharmaceuticals Inc
Novel time-dependent inhibitors of human placental aromatase.
Marion Merrell Dow Research Institute
Inhibition of human placental aromatase by novel homologated 19-oxiranyl and 19-thiiranyl steroids.
Johns Hopkins University School of Medicine
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
Ciba-Geigy AG
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
Universität des Saarlandes
Aromatase inhibitors and apoptotic inducers: Design, synthesis, anticancer activity and molecular modeling studies of novel phenothiazine derivatives carrying sulfonamide moiety as hybrid molecules.
King Saud University
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.
Universität des Saarlandes
Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.
Merck Research Laboratories
Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity.
Health Sciences University of Hokkaido
Conformational analysis of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione (rogletimide) and discovery of potent 5-alkyl derivatives.
Institute of Cancer Research
Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists
Uppsala University
The Synthesis and Evaluation of C7-Substituted a-Tetralone Derivatives as Inhibitors of Monoamine Oxidase.
North-West University
Identification of a novel hypothalamic neuropeptide Y receptor associated with feeding behavior.
Bayer Corporation
Molecular cloning and expression of a dopamine D2 receptor from human retina.
National Institute of Neurological Disorders and Stroke
URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices.
University of California Irvine
Inverse in silico screening for identification of kinase inhibitor targets.
University of Munich
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Development of pyridopyrimidines as potent Akt1/2 inhibitors.
Merck Research Laboratories
Structure-activity study of brassinin derivatives as indoleamine 2,3-dioxygenase inhibitors.
Bryn Mawr College
Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors.
Bryn Mawr College
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.
Amgen Inc
Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A.
University of Belgrade
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.
Genentech
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase.
Bryn Mawr College
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Astex
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.
MethylGene Inc
Chemically induced dimerization of human nonpancreatic secretory phospholipase A2 by bis-indole derivatives.
Peking University
N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.
Montana State University
Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening.
The Scripps Research Institute
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
VU University Amsterdam
2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice.
Biovitrum AB
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.
Friedrich Alexander University Erlangen