Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity

Bioorganic and Medicinal Chemistry Letters

Volumn 28, Issue 2, 2018, Pages 85-93

  Gong, Hua ^a   Weinstein, David S ^a   Lu, Zhonghui ^a   Duan, James J W ^a   Stachura, Sylwia ^a   Haque, Lauren ^a   Karmakar, Ananta ^a   Hemagiri, Hemalatha ^a   Raut, Dhanya Kumar ^a   Gupta, Arun Kumar ^a   Khan, Javed ^a   Camac, Dan ^a   Sack, John S ^a   Pudzianowski, Andrew ^a   Wu, Dauh Rurng ^a   Yarde, Melissa ^a   Shen, Ding Ren ^a   Borowski, Virna ^a   Xie, Jenny H ^a   Sun, Huadong ^a   D'Arienzo, Celia ^a   Dabros, Marta ^a   Galella, Michael A ^a   Wang, Faye ^a   Weigelt, Carolyn A ^a   Zhao, Qihong ^a   Foster, William ^a   Somerville, John E ^a   Salter Cid, Luisa M ^a   Barrish, Joel C ^a   Carter, Percy H ^a   Dhar, T G Murali ^a   more..

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BRIDGED BICYCLO COMPOUNDS; HEXAFLUORO 2 PROPANOL; LIVER X RECEPTOR; PREGNANE X RECEPTOR; PROPANOL; RETINOIC ACID RECEPTOR; RETINOIC ACID RECEPTOR GAMMA; STEROID RECEPTOR; SULFONAMIDE;

AGONISTS; ANIMAL; BAGG ALBINO MOUSE; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DESIGN; HUMAN; MALE; MOLECULAR MODEL; MOUSE; STRUCTURE ACTIVITY RELATION; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

ANIMALS; BRIDGED BICYCLO COMPOUNDS; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; HUMANS; LIVER X RECEPTORS; MALE; MICE; MICE, INBRED BALB C; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROPANOLS; RECEPTORS, RETINOIC ACID; RECEPTORS, STEROID; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 85037665317     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2017.12.006     Document Type: Article

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