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Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.
Tian, Yuan; Ma, Yao; Gibeau, Craig R; Lahue, Brian R; Shipps, Gerald W; Strickland, Corey; Bogen, Stéphane L.
  • Tian Y; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address: yuan.tian2@merck.com.
  • Ma Y; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Gibeau CR; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Lahue BR; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Shipps GW; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Strickland C; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Bogen SL; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 26(11): 2735-8, 2016 06 01.
Article en En | MEDLINE | ID: mdl-27080185
ABSTRACT
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53-hDM2 inhibitors was conducted. A structure-activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperidinas / Proteína p53 Supresora de Tumor / Proteínas Proto-Oncogénicas c-mdm2 / Leucina Límite: Humans Idioma: En Año: 2016 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piperidinas / Proteína p53 Supresora de Tumor / Proteínas Proto-Oncogénicas c-mdm2 / Leucina Límite: Humans Idioma: En Año: 2016 Tipo del documento: Article