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Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability.
Kawada, Hatsuo; Ebiike, Hirosato; Tsukazaki, Masao; Yamamoto, Shun; Koyama, Kohei; Nakamura, Mitsuaki; Morikami, Kenji; Yoshinari, Kiyoshi; Yoshida, Miyuki; Ogawa, Kotaro; Shinma, Nobuo; Tsukuda, Takuo; Ohwada, Jun.
Afiliação
  • Kawada H; Research Division, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. Electronic address: kawadahto@chugai-pharm.co.jp.
  • Ebiike H; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Tsukazaki M; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Yamamoto S; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Koyama K; Research Division, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan.
  • Nakamura M; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Morikami K; Research Division, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan.
  • Yoshinari K; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Yoshida M; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Ogawa K; Research Division, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan.
  • Shinma N; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Tsukuda T; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
  • Ohwada J; Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
Bioorg Med Chem ; 23(24): 7650-60, 2015 Dec 15.
Article em En | MEDLINE | ID: mdl-26613634
ABSTRACT
Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Pirróis / Inibidores de Proteínas Quinases / Inibidores de Fosfoinositídeo-3 Quinase Limite: Animals / Female / Humans / Male Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Pirróis / Inibidores de Proteínas Quinases / Inibidores de Fosfoinositídeo-3 Quinase Limite: Animals / Female / Humans / Male Idioma: En Ano de publicação: 2015 Tipo de documento: Article