Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy

Bioorganic and Medicinal Chemistry Letters

Volumn 28, Issue 12, 2018, Pages 2159-2164

  Lu, Tianbao ^a   Schubert, Carsten ^a   Cummings, Maxwell D ^a   Bignan, Gilles ^a   Connolly, Peter J ^a   Smans, Karine ^a   Ludovici, Donald ^a   Parker, Michael H ^a   Meyer, Christophe ^a   Rocaboy, Christian ^b   Alexander, Richard ^a   Grasberger, Bruce ^a   De Breucker, Sabine ^a   Esser, Norbert ^a   Fraiponts, Erwin ^a   Gilissen, Ron ^a   Janssens, Boudewijn ^a   Peeters, Danielle ^a   Van Nuffel, Luc ^a   Vermeulen, Peter ^a   Bischoff, James ^a   Meerpoel, Lieven ^a   more..

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^b VillaPharma Research   (Spain)

Author keywords

Cancer; Cell proliferation; Enzyme inhibitor; Fatty acid synthase; SAR; X ray crystal structure

Indexed keywords

FATTY ACID SYNTHASE INHIBITOR; MALONYL COENZYME A; PALMITIC ACID; ANTINEOPLASTIC AGENT; ENZYME INHIBITOR; FASN PROTEIN, HUMAN; FATTY ACID SYNTHASE; IMIDAZOLE DERIVATIVE;

A2780 CELL LINE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROLIFERATIVE ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER THERAPY; CELL SPECIFICITY; CHEMICAL MODIFICATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG DOSE COMPARISON; DRUG EXPOSURE; DRUG HALF LIFE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; LNCAP CELL LINE; MAXIMUM CONCENTRATION; MICROSOME; MOUSE; NCI-H460 CELL LINE; NONHUMAN; PC-3M CELL LINE; PHARMACODYNAMICS; PLASMA PROTEIN BINDING; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION; TISSUE LEVEL; TUMOR XENOGRAFT; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL PROLIFERATION; CHEMICAL STRUCTURE; DRUG EFFECT; DRUG SCREENING; EXPERIMENTAL NEOPLASM; METABOLISM; MOLECULAR MODEL; PATHOLOGY; SYNTHESIS;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; ENZYME INHIBITORS; FATTY ACID SYNTHASE, TYPE I; HUMANS; IMIDAZOLES; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPLASMS, EXPERIMENTAL; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85047095411     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2018.05.014     Document Type: Article

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