Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.

Papillon, Julien P N; Nakajima, Katsumasa; Adair, Christopher D; Hempel, Jonathan; Jouk, Andriana O; Karki, Rajeshri G; Mathieu, Simon; Möbitz, Henrik; Ntaganda, Rukundo; Smith, Troy; Visser, Michael; Hill, Susan E; Hurtado, Felipe Kellermann; Chenail, Gregg; Bhang, Hyo-Eun C; Bric, Anka; Xiang, Kay; Bushold, Geoffrey; Gilbert, Tamara; Vattay, Anthony; Dooley, Julie; Costa, Emily A; Park, Isabel; Li, Ailing; Farley, David; Lounkine, Eugen; Yue, Q Kimberley; Xie, Xiaoling; Zhu, Xiaoping; Kulathila, Raviraj; King, Daniel; Hu, Tiancen; Vulic, Katarina; Cantwell, John; Luu, Catherine; Jagani, Zainab

Papillon, Julien P N; Nakajima, Katsumasa; Adair, Christopher D; Hempel, Jonathan; Jouk, Andriana O; Karki, Rajeshri G; Mathieu, Simon; Möbitz, Henrik; Ntaganda, Rukundo; Smith, Troy; Visser, Michael; Hill, Susan E; Hurtado, Felipe Kellermann; Chenail, Gregg; Bhang, Hyo-Eun C; Bric, Anka; Xiang, Kay; Bushold, Geoffrey; Gilbert, Tamara; Vattay, Anthony; Dooley, Julie; Costa, Emily A; Park, Isabel; Li, Ailing; Farley, David; Lounkine, Eugen; Yue, Q Kimberley; Xie, Xiaoling; Zhu, Xiaoping; Kulathila, Raviraj; King, Daniel; Hu, Tiancen; Vulic, Katarina; Cantwell, John; Luu, Catherine; Jagani, Zainab.

Affiliation

Möbitz H; Global Discovery Chemistry , Novartis Institutes for Biomedical Research , Basel 4002 , Switzerland.
Cantwell J; Novartis Institutes for Biomedical Research , 5300 Chiron Way , Emeryville , California 94608 , United States.
Luu C; Novartis Institutes for Biomedical Research , 5300 Chiron Way , Emeryville , California 94608 , United States.

J Med Chem ; 61(22): 10155-10172, 2018 11 21.

Article in En | MEDLINE | ID: mdl-30339381

Subject(s)

Antineoplastic Agents/administration & dosage; Antineoplastic Agents/pharmacology; DNA Helicases/genetics; Drug Design; Mutation; Nuclear Proteins/genetics; Transcription Factors/antagonists & inhibitors; Transcription Factors/genetics; Administration, Oral; Animals; Antineoplastic Agents/chemistry; Cell Line, Tumor; Dose-Response Relationship, Drug; Humans; Mice; Models, Molecular; Protein Conformation; Structure-Activity Relationship; Transcription Factors/chemistry; Xenograft Model Antitumor Assays

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Transcription Factors / Nuclear Proteins / Drug Design / DNA Helicases / Mutation / Antineoplastic Agents Type of study: Prognostic_studies Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2018 Type: Article

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