Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP)

Journal of Medicinal Chemistry

Volumn 57, Issue 7, 2014, Pages 3053-3074

  Jansen, Koen ^a   Heirbaut, Leen ^a   Verkerk, Robert ^a   Cheng, Jonathan D ^b   Joossens, Jurgen ^a   Cos, Paul ^a   Maes, Louis ^a   Lambeir, Anne Marie ^a   De Meester, Ingrid ^a   Augustyns, Koen ^a   Van Der Veken, Pieter ^a  

^a UNIVERSITY OF ANTWERP   (Belgium)

^b FOX CHASE CANCER CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(4 QUINOLINOYL)GLYCYL 2 CYANOPYRROLIDINE; 1 [2 (QUINOLINE 4 CARBOXAMIDO)ACETYL]PYRROLIDIN 2 YL BORONIC ACID; 4 AMINO N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL]BENZAMIDE; 4 AMINO N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL]BENZAMIDE 2,2,2 TRIFLUOROACETATE; 5 BROMO N[2 (2 CYANO 4,4 DIFLUOROPYRROLIDIN 1 YL) 2 OXOETHYL]QUINOLINE 4 CARBOXAMIDE; 5 CYANO N[2 (2 CYANO 4,4 DIFLUOROPYRROLIDIN 1 YL) 2 OXOETHYL]QUINOLINE 4 CARBOXAMIDE; FIBROBLAST ACTIVATION PROTEIN; N[2 ((2,4) 2 CYANO 4 FLUOROPYRROLIDIN 1 YL) 2 OXOETHYL]QUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANO 4,4 DIFLUOROPYRROLIDIN 1 YL) 2 OXOETHYL] 6 METHOXYQUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANO 4,4 DIFLUOROPYRROLIDIN 1 YL) 2 OXOETHYL]QUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 1,7 NAPHTHYRIDINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 1H PYRROLO[2,3 B]PYRIDINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 2 (4 FLUOROPHENYL) 3H IMIDAZO[4,5 B]PYRIDINE 7 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 2 (4 METHOXYPHENYL) 3H IMIDAZO[4,5 B]PYRIDINE 7 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 4 (2,2,2 TRIFLUOROACETAMIDO)BENZAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 4 (2,2,2 TRIFLUOROACETAMIDO)BENZAMIDEI; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 4 METHYLOXAZOLE 5 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 5 METHOXYQUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 5 METHYLQUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 5 PHENYLQUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 7 (PHENYLAMINO)QUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 7 METHYLQUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL] 7 PHENYLQUINOLINE 4 CARBOXAMIDE; N[2 (2 CYANOPYRROLIDIN 1 YL) 2 OXOETHYL][1,2,4]TRIAZOLO[1,5 A]PYRIMIDINE 7 CARBOXAMIDE; N[2 OXO 2 (PYRROLIDIN 1 YL)ETHYL]QUINOLINE 4 CARBOXAMIDE; N[2 [2 (2 CHLOROACETYL)PYRROLIDIN 1 YL] 2 OXOETHYL]QUINOLINE 4 CARBOXAMIDE; N[2 [2 (2,4) 2 CYANO 4 FLUOROPYRROLIDIN 1 YL] 2 OXOETHYL]QUINOLINE 4 CARBOXAMIDE; SERINE PROTEINASE; SERINE PROTEINASE INHIBITOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; MOUSE; NONHUMAN; PLASMA HALF LIFE; STRUCTURE ACTIVITY RELATION;

ANIMALS; BIOLOGICAL AVAILABILITY; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; GELATINASES; HUMANS; MEMBRANE PROTEINS; MICE; MICROSOMES; MOLECULAR STRUCTURE; PLASMA; PYRROLIDINES; SERINE ENDOPEPTIDASES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION;

EID: 84898426099     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500031w     Document Type: Article

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