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Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity.
Imaizumi, Tomoyoshi; Akaiwa, Michinori; Abe, Tomoaki; Nigawara, Takahiro; Koike, Takanori; Satake, Yoshiki; Watanabe, Kazushi; Kaneko, Osamu; Amano, Yasushi; Mori, Kenichi; Yamanaka, Yosuke; Nagashima, Takeyuki; Shimazaki, Masashi; Kuramoto, Kazuyuki.
Afiliação
  • Imaizumi T; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. Electronic address: tomoyoshi.imaizumi@astellas.com.
  • Akaiwa M; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Abe T; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Nigawara T; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Koike T; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Satake Y; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Watanabe K; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Kaneko O; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Amano Y; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Mori K; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Yamanaka Y; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Nagashima T; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Shimazaki M; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
  • Kuramoto K; Tsukuba Research Center, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
Bioorg Med Chem ; 71: 116949, 2022 10 01.
Article em En | MEDLINE | ID: mdl-35926326
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Proteínas Proto-Oncogênicas p21(ras) / Alcanos / Neoplasias Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Proteínas Proto-Oncogênicas p21(ras) / Alcanos / Neoplasias Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article