Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation.

Kawada, Hatsuo; Ebiike, Hirosato; Tsukazaki, Masao; Nakamura, Mitsuaki; Morikami, Kenji; Yoshinari, Kiyoshi; Yoshida, Miyuki; Ogawa, Kotaro; Shimma, Nobuo; Tsukuda, Takuo; Ohwada, Jun

Kawada, Hatsuo; Ebiike, Hirosato; Tsukazaki, Masao; Nakamura, Mitsuaki; Morikami, Kenji; Yoshinari, Kiyoshi; Yoshida, Miyuki; Ogawa, Kotaro; Shimma, Nobuo; Tsukuda, Takuo; Ohwada, Jun.

Affiliation

Kawada H; Research Division, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. kawadahto@chugai-pharm.co.jp

Bioorg Med Chem Lett ; 23(3): 673-8, 2013 Feb 01.

Article in En | MEDLINE | ID: mdl-23265889

Subject(s)

Glucuronic Acid/chemistry; Phenols/chemistry; Phosphoinositide-3 Kinase Inhibitors; Pyrimidines/chemical synthesis; Pyrroles/chemical synthesis; Animals; Breast Neoplasms/drug therapy; Cell Line, Tumor; Crystallography, X-Ray; Enzyme Activation/drug effects; Female; Humans; Hydrogen Bonding; Inhibitory Concentration 50; Mice; Molecular Structure; Pyrimidines/chemistry; Pyrimidines/pharmacology; Pyrroles/chemistry; Pyrroles/pharmacology; Structure-Activity Relationship; Xenograft Model Antitumor Assays

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Phenols / Pyrimidines / Pyrroles / Glucuronic Acid / Phosphoinositide-3 Kinase Inhibitors Type of study: Prognostic_studies Limits: Animals / Female / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Type: Article Affiliation country: Japan

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