Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 15, 2012, Pages 5114-5117

  Liu, Kevin K C ^a   Bailey, Simon ^a   Dinh, Dac M ^a   Lam, Hieu ^a   Li, Chunze ^a   Wells, Peter A ^a   Yin, Min Jean ^a   Zou, Aihua ^a  

^a PFIZER INC   (United States)

Author keywords

Conformationally restricted; Kinase inhibitors; mTOR; Oncology

Indexed keywords

MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PF 05139962; SULFONE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG ACTIVITY; DRUG CONFORMATION; DRUG POTENCY; DRUG SELECTIVITY; ENZYME INHIBITION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING SITES; COMPUTER SIMULATION; HALF-LIFE; HUMANS; MICROSOMES, LIVER; MORPHOLINES; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; TOR SERINE-THREONINE KINASES;

EID: 84863984121     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.05.104     Document Type: Article

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