PMID

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Article Title

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Antihyperlipidemic morpholine derivatives with antioxidant activity: An investigation of the aromatic substitution.

University of Athens

Multitarget drug discovery for tuberculosis and other infectious diseases.

University of Illinois At Urbana-Champaign

Design of novel potent antihyperlipidemic agents with antioxidant/anti-inflammatory properties: exploiting phenothiazine's strong antioxidant activity.

University of Athens

Discovery of DF-461, a Potent Squalene Synthase Inhibitor.

Daiichi Sankyo

New multifunctional Di-tert-butylphenoloctahydro(pyrido/benz)oxazine derivatives with antioxidant, antihyperlipidemic, and antidiabetic action.

University of Athens

Head-to-head prenyl tranferases: anti-infective drug targets.

University of Illinois At Urbana-Champaign

Discovery of novel tricyclic compounds as squalene synthase inhibitors.

Daiichi Sankyo

Kinetic characterization of squalene synthase from Trypanosoma cruzi: selective inhibition by quinuclidine derivatives.

Instituto De Parasitolog£A Y Biomedicina&Quot;L£Pez-Neyra

Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.

Bristol-Myers Squibb Pharmaceutical Research Institute

 

N-Hydroxyglycine derivatives as novel inhibitors of squalene synthase

TBA

 

Synthesis and biological activity of J-104,118, a novel, potent inhibitor of squalene synthase

TBA

 

Aromatic isosteres as conformational probes for an isoprenyl subunit: application to inhibitors of squalene synthase

TBA

 

The squalestatins: potent inhibitors of squalene synthase. The role of the tricarboxylic acid moiety.

TBA

 

Synthesis and squalene synthetase inhibitory activity of tripotassium 1-methyl-1-[(N-benzyl-N-farnesyl)aminoethylphosphinato]ethylphosphonate as a tethered analog of N-benzyl-N-farnesylamine-inorganic pyrophosphate ion pair

TBA

Novel benzoxazine and benzothiazine derivatives as multifunctional antihyperlipidemic agents.

University of Athens

Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: novel, highly potent and orally efficacious squalene synthase inhibitors.

Daiichi Sankyo

Identification of 4H,6H-[2]benzoxepino[4,5-c][1,2]oxazoles as novel squalene synthase inhibitors.

Bayer Pharma

Identification and optimization of tetrahydro-2H-3-benzazepin-2-ones as squalene synthase inhibitors.

Bayer Pharma

Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors.

Daiichi Sankyo

Design of more potent squalene synthase inhibitors with multiple activities.

University of Athens

Synthesis and preliminary pharmacological characterisation of a new class of nitrogen-containing bisphosphonates (N-BPs).

Universit£

Phosphonosulfonates are potent, selective inhibitors of dehydrosqualene synthase and staphyloxanthin biosynthesis in Staphylococcus aureus.

University of Illinois At Urbana-Champaign

Zaragozic Acids D and D₂: Potent Inhibitors of Squalene Synthase and of Ras Farnesyl-Protein Transferase

TBA

 

Novel Zaragozic Acids from Leptodontidium elatius

TBA

 

Rhombenone: farnesyl protein transferase inhibitor from the leaves of Hedera rhombea Bean

TBA

 

Novel optimised quinuclidine squalene synthase inhibitors

TBA

 

Synthesis of triphosphonate analogues of farnesyl pyrophosphate. Inhibitors of squalene synthase and protein:farnesyl transferase

TBA

 

J-104,123, a novel and orally-active inhibitor of squalene synthase: Stereoselective synthesis and cholesterol lowering effects in dogs

TBA

 

Sulfobetaine zwitterionic inhibitors of squalene synthase

TBA

 

Squalene synthase inhibitors: isosteric replacements of the farnesyl chain of benzyl farnesyl amine

TBA

 

Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine

TBA

 

Isolation, structure determination and squalene synthase activity of L-731,120 and L-731,128, alkyl citrate analogs of zaragozic acids A and B

TBA

 

3,4-Diesters of zaragozic acid A

TBA

 

Structurally simplified squalestatins: monocyclic 1,3-dioxane analogues.

TBA

 

The squalestatins: effects of changes at the allylic centre in the C1 sidechain

TBA

 

Synthesis of novel monocyclic squalestatin analogues as potential inhibitors of squalene synthase

TBA

 

The squalestatins: Potent inhibitors of squalene synthase, 3-hydroxymethyl derivatives.

TBA

 

Design and synthesis of squalene synthase inhibitors - acylic mimics of the zaragazic acids

TBA

 

Semi-synthetic qualestatins: Squalene synthase inhibition and antifungal activity. The SAR of C6 and C7 modifications

TBA

 

The squalestatins: novel inhibitors of squalene synthase. The optimal C1 chain-length requirements.

TBA

 

Diesters of zaragozic acid A: Synthesis and biological activity

TBA

Inhibition of staphyloxanthin virulence factor biosynthesis in Staphylococcus aureus: in vitro, in vivo, and crystallographic results.

University of Illinois At Urbana-Champaign

Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity.

University of Athens

Quinuclidine derivatives as potential antiparasitics.

Cardiff University

Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole.

Instituto Venezolano De Investigaciones CientíFicas

Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.

University of Illinois At Urbana-Champaign

Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis.

Takeda Chemical Industries

Novel reverse-turn mimics inhibit farnesyl transferase.

Cold Spring Harbor Laboratory

Quinuclidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase: optimization from lipid profiles.

Zeneca Pharmaceuticals

Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.

Abbott Laboratories

(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.

Abbott Laboratories

Optimizing the Pharmacological Profile of New Bifunctional Antihyperlipidemic/Antioxidant Morpholine Derivatives.

University of Athens

Synthesis and activity of a novel series of 3-biarylquinuclidine squalene synthase inhibitors.

Zeneca Pharmaceuticals

The squalestatins: inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C3-modified analogues.

Glaxo Wellcome Research and Development

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Amidinium cation as a mimic of allylic carbocation: synthesis and squalene synthetase inhibitory activity of an amidinium analog of a carbocation intermediate.

Sandoz Research Institute

N-(arylalkyl)farnesylamines: new potent squalene synthetase inhibitors.

Sandoz Research Institute

Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives.

Merck Research Laboratories

The squalestatins: novel inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C1-modified analogues.

Glaxo Research and Development

The squalestatins: synthesis and biological activity of some C3-modified analogues; replacement of a carboxylic acid or methyl ester with an isoelectronic heterocyclic functionality.

Glaxo Research and Development

1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate.

Bristol-Myers Squibb Pharmaceutical Research Institute

Phenoxypropylamines: a new series of squalene synthase inhibitors.

Zeneca Pharmaceuticals

Developing potential agents against atherosclerosis: Design, synthesis and pharmacological evaluation of novel dual inhibitors of oxidative stress and Squalene Synthase activity.

National and Kapodistrian University of Athens