PMID

Data

Article Title

Organization

Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?

Merck Research Laboratories

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

Surfing the piperazine core of tricyclic farnesyltransferase inhibitors.

Pharmacopeia

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

Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.

Yale University

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

Design and synthesis of potent nonpeptidic farnesyltransferase inhibitors based on a terphenyl scaffold.

Yale University

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

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

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

Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.

Schering-Plough Research Institute

Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.

Schering-Plough Research Institute

Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I.

Yale University

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

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

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