Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2- phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a] pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 15, 2011, Pages 4429-4435

  Kinzel, Olaf ^a   Alfieri, Anna ^a   Altamura, Sergio ^a   Brunetti, Mirko ^a   Bufali, Simone ^a   Colaceci, Fabrizio ^a   Ferrigno, Federica ^a   Filocamo, Gessica ^a   Fonsi, Massimiliano ^a   Gallinari, Paola ^a   Malancona, Savina ^a   Hernando, Jose Ignacio Martin ^a   Monteagudo, Edith ^a   Orsale, Maria Vittoria ^a   Palumbi, Maria Cecilia ^a   Pucci, Vincenzo ^a   Rowley, Michael ^a   Sasso, Romina ^a   Scarpelli, Rita ^a   Steinkühler, Christian ^a   Jones, Philip ^a   more..

^a IRBM   (Italy)

Author keywords

Hedgehog inhibitor; Hedgehog pathway; Smoothened antagonist

Indexed keywords

8A METHYL 1,3 DIOXO 2 (2 PHENYLCYCLOPROPYL) N (1 PHENYL 1H PYRAZOL 5 YL)HEXAHYDRO IMIDAZO[1,5 A]PYRAZINE 7 (1H)CARBOXAMIDE; ANTINEOPLASTIC AGENT; HYDANTOIN DERIVATIVE; MK 5710; TETRAHYDROIMIDAZO [1,5 A]PYRAZINE 1,3 (2H,5H)DIONE; UNCLASSIFIED DRUG;

ALKYLATION; ALLOGRAFT; ANIMAL CELL; ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; EPIMERIZATION; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; NONHUMAN; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTINEOPLASTIC AGENTS; DOGS; HEDGEHOG PROTEINS; HUMANS; IMIDAZOLES; MICE; NEOPLASMS; PYRAZINES; RATS; SIGNAL TRANSDUCTION; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

ERINACEIDAE;

EID: 79960349060     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.06.023     Document Type: Article

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