Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective αvβ3 inhibitor: Design, synthesis, and optimization

Bioorganic and Medicinal Chemistry

Volumn 15, Issue 10, 2007, Pages 3390-3412

  Nagarajan, Srinivasan R ^a   Lu, Hwang Fun ^a   Gasiecki, Alan F ^a   Khanna, Ish K ^a   Parikh, Mihir D ^a   Desai, Bipinchandra N ^a   Rogers, Thomas E ^a   Clare, Michael ^a   Chen, Barbara B ^a   Russell, Mark A ^a   Keene, Jeffery L ^a   Duffin, Tiffany ^a   Engleman, V Wayne ^a   Finn, Mary B ^a   Freeman, Sandra K ^a   Klover, Jon A ^a   Nickols, G Alan ^a   Nickols, Maureen A ^a   Shannon, Kristen E ^a   Steininger, Christina A ^a   Westlin, William F ^a   Westlin, Marisa M ^a   Williams, Melanie L ^a   more..

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Angiogenesis; Antagonists; Avb3; Cyclopropyl; Integrin receptors; RGD mimics

Indexed keywords

1 PHENYL 2 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYLACETIC ACID; 2 [2 (4 METHOXYPHENYL) 2 METHYLCYCLOPROPYL]ETHANOL; 2 [4 [3 (2 PYRIDINYLAMINO)PROPOXY]PHENYL]CYCLOPROPANEACETIC ACID; 2,2 DIMETHYL 3 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYLACETIC ACID; 3 [2 [3 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]PROPIONIC ACID; 3 [2 [4 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YLMETHOXY)PHENYL]CYCLOPROPYL]PROPIONIC ACID; 3 [2 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]PROPIONIC ACID; 4 [3 (2 N PYRIDYL)AMINO] 1 PROPYLOXYPHENYL 3 (3 PYRIDYL)BUTYRIC ACID; [2 [2,3 DIFLUORO 4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID TRIFLUOROACETATE; [2 [3 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2 [3 FLUORO 4 [3 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YLAMINO)PROPOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2 [3 HYDROXY 4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2 [4 [2 [6 (METHYLAMINO)PYRIDIN 2 YL]ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2 [6 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PYRIDIN 3 YL]CYCLOPROPYL]ACETIC ACID; [2 METHYL 2 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2,2 DIBROMO 3 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2,2 DICHLORO 3 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; [2,2 DIMETHYL 3 [4 [2 (5,6,7,8 TETRAHYDRO 1,8 NAPHTHYRIDIN 2 YL)ETHOXY]PHENYL]CYCLOPROPYL]ACETIC ACID; ACETIC ACID DERIVATIVE; ETHYL 3 [2 (4 HYDROXYPHENYL)CYCLOPROPYL]PROPIONIC ACID; ETHYL[2 (4 HYDROXYPHENYL) 2 METHYLCYCLOPROPYL]ACETIC ACID; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; VITRONECTIN RECEPTOR;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COLON CARCINOMA; CONTROLLED STUDY; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MALE; MOUSE; NONHUMAN; PROCESS OPTIMIZATION; RAT; SUBSTITUTION REACTION;

ACETIC ACIDS; ANIMALS; AREA UNDER CURVE; CELL LINE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HALF-LIFE; HUMANS; INDICATORS AND REAGENTS; INTEGRIN ALPHAVBETA3; MALE; MICE; NAPHTHYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; SPECTROPHOTOMETRY, ULTRAVIOLET; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION;

EID: 34047105798     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2007.03.020     Document Type: Article

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