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

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 3, 2013, Pages 673-678

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

^a CHUGAI PHARMACEUTICAL CO LTD   (Japan)

Author keywords

Bioisostere; Cancer; Glucuronic acid conjugation; PI3K; SBDD

Indexed keywords

AMINOPYRIMIDINE DERIVATIVE; ANTINEOPLASTIC AGENT; GLUCURONIC ACID; PHENOL DERIVATIVE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BREAST CANCER; CANCER CELL CULTURE; CANCER INHIBITION; CONTROLLED STUDY; DRUG CLEARANCE; DRUG CONJUGATION; DRUG GLUCURONIDATION; DRUG HALF LIFE; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; HYDROGEN BOND; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOLECULAR DOCKING; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

ANIMALS; BREAST NEOPLASMS; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; ENZYME ACTIVATION; FEMALE; GLUCURONIC ACID; HUMANS; HYDROGEN BONDING; INHIBITORY CONCENTRATION 50; MICE; MOLECULAR STRUCTURE; PHENOLS; PHOSPHATIDYLINOSITOL 3-KINASES; PYRIMIDINES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84872291663     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.11.112     Document Type: Article

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