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Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.
Barberis, Claude; Erdman, Paul; Czekaj, Mark; Fire, Luke; Pribish, James; Tserlin, Elina; Maniar, Sachin; Batchelor, Joseph D; Liu, Jinyu; Patel, Vinod F; Hebert, Andrew; Levit, Mikhail; Wang, Anlai; Sun, Frank; Huang, Shih-Min A.
Afiliação
  • Barberis C; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States. Electronic address: claude.barberis2@sanofi.com.
  • Erdman P; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States; Present address: AbbVie, 100 Abbott Park Road, Abbott Park, IL 60064-3500, United States.
  • Czekaj M; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States.
  • Fire L; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States; Present address: Rakuten Medical, 11080 Roselle St, San Diego, CA 92121, United States.
  • Pribish J; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States.
  • Tserlin E; Present address: Qiagen, 561 Virginia Road, Concord, MA 01742, United States.
  • Maniar S; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States.
  • Batchelor JD; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States.
  • Liu J; IDD Medicinal Chemistry, Sanofi, 153 Second Avenue, Waltham MA 02451, United States.
  • Patel VF; Present address: TME Therapeutics, 3 Mossy Lane, Acton, MA 01720, United States.
  • Hebert A; Oncology Biochemistry, Sanofi, 270 Albany Street, Cambridge MA 02139, United States.
  • Levit M; Oncology Biochemistry, Sanofi, 270 Albany Street, Cambridge MA 02139, United States.
  • Wang A; Oncology Biology, Sanofi, 270 Albany Street, Cambridge MA 02139, United States.
  • Sun F; Oncology Pharmacology, Sanofi, 640 Memorial Drive, Cambridge MA 02139, United States.
  • Huang SA; Oncology Biology, Sanofi, 270 Albany Street, Cambridge MA 02139, United States; Present address: Bristol-Myers Squibb, 3551 Lawrenceville Princeton, Lawrence Township, NJ 08648, United States.
Bioorg Med Chem Lett ; 30(23): 127625, 2020 12 01.
Article em En | MEDLINE | ID: mdl-33096160
ABSTRACT
N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which subsequently impacted KG-1 tumor growth in a mouse model.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Aza / Inibidores de Proteínas Quinases / Indóis / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Aza / Inibidores de Proteínas Quinases / Indóis / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article