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Article Title

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Investigation of fluorinated and bifunctionalized 3-phenylchroman-4-one (isoflavanone) aromatase inhibitors.

Northern Kentucky University

Pyrrolizines: Promising scaffolds for anticancer drugs.

Beni-Suef 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

Synthesis and bioconversions of formestane.

The University Of Tampa

Chemopreventive and antioxidant activity of 6-substituted imidazo[2,1-b]thiazoles.

Universit£

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

Analogues of aminoglutethimide: selective inhibition of aromatase.

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

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

Is there a case for P-450 inhibitors in cancer treatment?

Janssen Research Foundation

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£

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

Bioactive compounds from the fern Lepisorus contortus.

Yunnan Normal University

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

 

The synthesis of N-aryl androsterone pyrazoles as aromatase inhibitors

TBA

 

Synthesis of 7α-substituted androstenediones by a 1,4-conjugate addition approach

TBA

 

Molecular modelling of inhibitors of aromatase — a novel approach

TBA

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

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

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

Aromatase inhibitors from Broussonetia papyrifera.

University Of Illinois At Chicago

Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.

TBA

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

Pyrazole and isoxazole derivatives as new, potent, and selective 20-hydroxy-5,8,11,14-eicosatetraenoic acid synthase inhibitors.

Taisho Pharmaceutical

Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.

Ufr Des Sciences Pharmaceutiques

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

Synthesis and evaluation of 17-aliphatic heterocycle-substituted steroidal inhibitors of 17alpha-hydroxylase/C17-20-lyase (P450 17).

University Of The Saarland

1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.

Cardiff University

New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles.

Nantes

Design and synthesis of a new type of non steroidal human aromatase inhibitors.

Centre D'Etudes Et De Recherche Sur Le MéDicament De Normandie

6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.

University Of Minnesota

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

Tetrahydronaphthalenes: influence of heterocyclic substituents on inhibition of steroid enzymes P450 arom and P450 17.

UniversitäT De Saarlandes

Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.

Ciba-Geigy

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

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

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

New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.

UniversitäT Des Saarlandes

Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.

UniversitäT Des Saarlandes

Stereoisomers of ketoconazole: preparation and biological activity.

Syntex Research

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

A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines.

Eli Lilly

Targeting a prokaryotic protein in a eukaryotic pathogen: identification of lead compounds against cryptosporidiosis.

Brandeis University

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

Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.

Merck Research Laboratories

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

Design, synthesis, and biological evaluation of potent c-Met inhibitors.

Amgen

Potent cationic inhibitors of West Nile virus NS2B/NS3 protease with serum stability, cell permeability and antiviral activity.

University Of Queensland

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

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

Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides.

Michigan State University

Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor.

Gsk

Inhibition of adenosine deaminase by analogues of adenosine and inosine, incorporating a common heterocyclic base, 4(7)-amino-6(5)H-imidazo[4,5-d]pyridazin-7(4)one.

University Of Maryland Baltimore County

Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).

Bristol-Myers Squibb Pharmaceutical Research Institute

Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.

Wyeth Research

Inhibition of herpes simplex virus thymidine kinases by 2-phenylamino-6-oxopurines and related compounds: structure-activity relationships and antiherpetic activity in vivo.

Glsynthesis

Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.

Istituto Superiore Di Sanita

Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.

Bayer Healthcare Pharmaceuticals