Thienopyrimidine bisphosphonate (ThPBP) inhibitors of the human farnesyl pyrophosphate synthase: Optimization and characterization of the mode of inhibition

Journal of Medicinal Chemistry

Volumn 56, Issue 20, 2013, Pages 7939-7950

  Leung, Chun Yuen ^a   Park, Jaeok ^a   De Schutter, Joris W ^a   Sebag, Michael ^b   Berghuis, Albert M ^a   Tsantrizos, Youla S ^a  

^a MCGILL UNIVERSITY   (Canada)

^b ROYAL VICTORIA HOSPITAL   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

(((6 (4 (2,2 DIFLUOROCYCLOPROPYL)PHENYL)THIENO[2,3 D]PYRIMIDIN 4YL)AMINO)METHYLENE)DIPHOSPHONIC ACID; (((6 (4 (TRIFLUOROMETHYL)PHENYL)THIENO[2,3 D]PYRIMIDIN 4 YL)AMINO)METHYLENE)DIPHOSPHONIC ACID; (((6 (4 CYCLOPROPOXYPHENYL)THIENO[2,3 D]PYRIMIDIN 4 YL)AMINO)METHYLENE)DIPHOSPHONIC ACID; (((6 (4 CYCLOPROPYLPHENYL)THIENO[2,3 D]PYRIMIDIN 4 YL)AMINO)METHYLENE)DIPHOSPHONIC ACID; (((6 (4 ISOPROPOXYPHENYL)THIENO[2,3 D]PYRIMIDIN 4 YL)AMINO)METHYLENE)DIPHOSPHONIC ACID; (((6 (4 METHOXYPHENYL)THIENO[2,3 D]PYRIMIDIN 4 YL)AMINO)METHYLENE)DIPHOSPHONIC ACID; ANTINEOPLASTIC AGENT; BISPHOSPHONIC ACID DERIVATIVE; ENZYME INHIBITOR; FARNESYL DIPHOSPHATE; FARNESYLPYROPHOSPHATE SYNTHASE; HYDROXYAPATITE; RISEDRONIC ACID; THIENOPYRIMIDINE BISPHOSPHONATE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BONE MINERAL; CELL LINE; CRYSTALLOGRAPHY; DRUG ACTIVITY; DRUG BINDING; DRUG POTENCY; DRUG STRUCTURE; ENZYME ACTIVE SITE; ENZYME PHOSPHORYLATION; HYDROPHILICITY; MULTIPLE MYELOMA;

CATALYTIC DOMAIN; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DIPHOSPHATES; DIPHOSPHONATES; ENZYME INHIBITORS; GERANYLTRANSTRANSFERASE; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; PYRIMIDINES;

EID: 84886481421     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400946f     Document Type: Article

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