129 articles for thisTarget
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New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation.
Alexandru Ioan Cuza University
Highly improved antiparasitic activity after introduction of an N-benzylimidazole moiety on protein farnesyltransferase inhibitors.
Cnrs Upr2301
Novel indolizine derivatives with unprecedented inhibitory activity on human farnesyltransferase.
Alexandru Ioan Cuza University
Design, synthesis, and evaluation of sugar amino acid based inhibitors of protein prenyl transferases PFT and PGGT-1.
Leiden University
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of acyloxymethyl ester prodrugs of the transferable protein farnesyl transferase substrate farnesyl methylenediphosphonate.
University Of Kentucky
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
Merck Research Laboratories
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
Merck Research Laboratories
Design, synthesis, and pharmacological evaluation of new farnesyl protein transferase inhibitors.
Universit£
Novel farnesol and geranylgeraniol analogues: A potential new class of anticancer agents directed against protein prenylation.
Parke-Davis Pharmaceutical Research
Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.
Merck Research Laboratories
Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.
Merck Research Laboratories
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.
3-Dimensional Pharmaceuticals
Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.
Warner-Lambert
Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors.
University Of Pittsburgh
Cyclic acid anhydrides as a new class of potent, selective and non-peptidic inhibitors of geranylgeranyl transferase.
University College London
Aromatic farnesyl diphosphate analogues: vinyl triflate-mediated synthesis and preliminary enzymatic evaluation.
Wayne State University
2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.
Merck Research Laboratories
Grignard-mediated synthesis and preliminary biological evaluation of novel 3-substituted farnesyl diphosphate analogues.
Wayne State University
Peptidomimetic inhibitors of p21ras farnesyltransferase: Hydrophobic functionalization leads to disruption of p21ras membrane association in whole cells
TBA
Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.
Yale University
Synthesis of triphosphonate analogues of farnesyl pyrophosphate. Inhibitors of squalene synthase and protein:farnesyl transferase
TBA
A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli
TBA
Oreganic acid: a potent novel inhibitor of ras farnesyl-protein transferase from an endophytic fungus
TBA
Rational design of potent carboxylic acid based bisubstrate inhibitors of ras farnesyl protein transferase
TBA
Hydantoin derivatives as non-peptidic inhibitors of Ras farnesyl transferase.
Keimyung University
Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.
Schering-Plough Research Institute
Guiding farnesyltransferase inhibitors from an ECLiPS library to the catalytic zinc.
Pharmacopeia
Novel triazole based inhibitors of Ras farnesyl transferase.
Janssen Research Foundation
Novel beta-(imidazol-4-yl)-beta-amino acids: solid-phase synthesis and study of their inhibitory activity against geranylgeranyl protein transferase type I.
Janssen Research Foundation
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Abbott Laboratories
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
Schering-Plough Research Institute
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Abbott Laboratories
Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.
Institut De Recherches Servier
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.
Yale University
Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity.
Università
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&Jprd)
4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.
Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&Jprd)
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Abbott Laboratories
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
Abbott Laboratories
Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I.
Imperial College
Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide.
Kyowa Hakko Kogyo
Antifungal activity of a Candida albicans GGTase I inhibitor-alanine conjugate. Inhibition of Rho1p prenylation in C. albicans.
Gpc Biotech
5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase.
Centre De Recherche Pierre Fabre
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Abbott Laboratories
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Abbott Laboratories
Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.
Schering-Plough Research Institute
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Merck Research Laboratories
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
A new class of type I protein geranylgeranyltransferase (GGTase I) inhibitor.
Banyu Tsukuba Research Institute
Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.
Schering-Plough Research Institute
Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.
Yale University
A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase).
Lgci
3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors.
Lgci
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Merck Research Laboratories
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity.
Yale University
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Merck Research Laboratories
Non-peptidic, non-prenylic inhibitors of the prenyl protein-specific protease Rce1.
Philipps-UniversitäT Marburg
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Multivariate data analysis using D-optimal designs, partial least squares, and response surface modeling: A directional approach for the analysis of farnesyltransferase inhibitors.
RhôNe-Poulenc Rorer
3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines, a novel series of farnesyltransferase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.
Bristol-Myers Squibb Pharmaceutical Research Institute
N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.
Merck Research Laboratories
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Schering-Plough Research Institute
Analogs of 4-(3-bromo-8-methyl-10-methoxy-6,11-dihydro-5H-benzo[5,6]-cyclo hepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N-oxide as inhibitors of farnesyl protein transferase.
Schering-Plough Research Institute
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.
Schering-Plough Research Institute
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.
Abbott Laboratories
Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.
Yale University
Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.
Abbott Laboratories
Pharmaceutical significance of azepane based motifs for drug discovery: A critical review.
Wuhan Institute Of Technology
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
Schering-Plough Research Institute
Kampanols: novel Ras farnesyl-protein transferase inhibitors from Stachybotrys kampalensis.
Merck Research Laboratories
Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.
Schering-Plough Research Institute
Design, synthesis, and biological evaluation of novel pyrrolo[1,2-a]pyrazine derivatives.
Yonsei University
Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.
Schering-Plough Research Institute
Structure-activity relationship of 3-substituted N-(pyridinylacetyl)-4- (8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene )- piperidine inhibitors of farnesyl-protein transferase: design and synthesis of in vivo active antitumor compounds.
Schering-Plough Research Institute
Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.
Schering-Plough Research Institute
Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective.
Indian Institute Of Technology (Bhu)
Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.
Centre De Recherches De Vitry-Alfortville
Geranylgeranyl diphosphate-based inhibitors of post-translational geranylgeranylation of cellular proteins.
Università
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Merck Research Laboratories
Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.
Bristol-Myers Squibb Pharmaceutical Research Institute
Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds.
Alexandru Ioan Cuza University
Farnesyltransferase inhibitors: CAAX mimetics based on different biaryl scaffolds.
Universit£
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
University Of Minnesota
New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.
Merck Research Laboratories
Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors.
'Al. I. Cuza' University Of Iasi
Neuroactive diol and acyloin metabolites from cone snail-associated bacteria.
University Of Utah
Peptidomimetic modification improves cell permeation of bivalent farnesyltransferase inhibitors.
Osaka University
Synthesis and biological evaluation of a new series of phenothiazine-containing protein farnesyltransferase inhibitors.
Al. I. Cuza University Of Iasi
Synthesis and biological evaluation of new phenothiazine derivatives bearing a pyrazole unit as protein farnesyltransferase inhibitors.
'Al. I. Cuza' University Of Iasi
New farnesyltransferase inhibitors in the phenothiazine series.
Al. I. Cuza University Of Iasi
Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues.
Centre De Recherche De Gif-Sur-Yvette
Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.
Chugai Pharmaceutical
Barceloneic acid A, a new farnesyl-protein transferase inhibitor from a Phoma species.
Merck Research Laboratories
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors.
Universit£
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.
University Of Washington
Synthesis, biochemical, and cellular evaluation of farnesyl monophosphate prodrugs as farnesyltransferase inhibitors.
Purdue University
3D-QSAR studies of farnesyltransferase inhibitors: a comparative molecular field analysis approach.
The M.S. University Of Baroda
Methyllucidone inhibits STAT3 activity by regulating the expression of the protein tyrosine phosphatase MEG2 in DU145 prostate carcinoma cells.
Korea University Of Science And Technology
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.
Temple University
New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis.
Centre De Recherche De Gif
Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.
Duke University Medical Center
Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.
Janssen Research Foundation
A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity.
Duke University Medical Center
(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
Schering-Plough Research Institute