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Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais, Gérald; Epple, Robert; Marsilje, Thomas H; Long, Yun O; McNeill, Matthew; Chen, Bei; Lu, Wenshuo; Anumolu, Jaganmohan; Badiger, Sangamesh; Bursulaya, Badry; DiDonato, Michael; Fong, Rina; Juarez, Jose; Li, Jie; Manuia, Mari; Mason, Daniel E; Gordon, Perry; Groessl, Todd; Johnson, Kevin; Jia, Yong; Kasibhatla, Shailaja; Li, Chun; Isbell, John; Spraggon, Glen; Bender, Steven; Michellys, Pierre-Yves.
Affiliation
  • Lelais G; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Epple R; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Marsilje TH; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Long YO; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • McNeill M; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Chen B; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Lu W; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Anumolu J; Aurigene Discovery Technologies , Bollaram Road, Miyapur, Hyderabad 500 049, India.
  • Badiger S; Aurigene Discovery Technologies , 39-40, Electronic City Phase 2, Bangalore 560 100, India.
  • Bursulaya B; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • DiDonato M; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Fong R; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Juarez J; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Li J; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Manuia M; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Mason DE; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Gordon P; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Groessl T; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Johnson K; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Jia Y; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Kasibhatla S; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Li C; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Isbell J; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Spraggon G; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Bender S; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
  • Michellys PY; Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.
J Med Chem ; 59(14): 6671-89, 2016 07 28.
Article in En | MEDLINE | ID: mdl-27433829
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzimidazoles / Carcinoma, Non-Small-Cell Lung / Protein Kinase Inhibitors / Drug Discovery / ErbB Receptors / Lung Neoplasms / Nicotine / Antineoplastic Agents Type of study: Prognostic_studies Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2016 Document type: Article Affiliation country: Country of publication:
Fulltext
Add to My VHL
Print
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PubMed Links
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzimidazoles / Carcinoma, Non-Small-Cell Lung / Protein Kinase Inhibitors / Drug Discovery / ErbB Receptors / Lung Neoplasms / Nicotine / Antineoplastic Agents Type of study: Prognostic_studies Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2016 Document type: Article Affiliation country: Country of publication: