Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 24, 2015, Pages 5743-5747

  Johannes, Jeffrey W ^a   Almeida, Lynsie ^a   Daly, Kevin ^a   Ferguson, Andrew D ^a   Grosskurth, Shaun E ^a   Guan, Huiping ^a   Howard, Tina ^a   Ioannidis, Stephanos ^a   Kazmirski, Steven ^a   Lamb, Michelle L ^a   Larsen, Nicholas A ^a   Lyne, Paul D ^a   Mikule, Keith ^a   Ogoe, Claude ^a   Peng, Bo ^a   Petteruti, Philip ^a   Read, Jon A ^a   Su, Nancy ^a   Sylvester, Mark ^a   Throner, Scott ^a   Wang, Wenxian ^a   Wang, Xin ^a   Wu, Jiaquan ^a   Ye, Qing ^a   Yu, Yan ^a   Zheng, Xiaolan ^a   Scott, David A ^a   more..

^a ASTRAZENECA   (United Kingdom)

Author keywords

Cell cycle; Centrosome; Oncology; PARP; Tankyrase

Indexed keywords

ANTINEOPLASTIC AGENT; AZ 0108; AZ 9482; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 1; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 2; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 3; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 6; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE INHIBITOR; TANKYRASE; TANKYRASE 1; TANKYRASE 2; UNCLASSIFIED DRUG; AZD108; PHTHALAZINE DERIVATIVE; TNKS PROTEIN, HUMAN;

ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CENTROSOME; DRUG BIOAVAILABILITY; FEMALE; HELA CELL LINE; HUMAN; HUMAN CELL; HYDROXYLATION; LIPOPHILICITY; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STEREOCHEMISTRY; ANIMAL; ANTAGONISTS AND INHIBITORS; BINDING SITE; CACO 2 CELL LINE; CHEMISTRY; CONFORMATION; DRUG EFFECTS; METABOLISM; MICROSOME; MOLECULAR DYNAMICS; ORAL DRUG ADMINISTRATION; PRECLINICAL STUDY; PROTEIN TERTIARY STRUCTURE; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; BINDING SITES; CACO-2 CELLS; CENTROSOME; CRYSTALLOGRAPHY, X-RAY; DRUG EVALUATION, PRECLINICAL; HELA CELLS; HUMANS; MICROSOMES; MOLECULAR CONFORMATION; MOLECULAR DYNAMICS SIMULATION; PHTHALAZINES; POLY(ADP-RIBOSE) POLYMERASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RATS; TANKYRASES;

EID: 84947266416     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.10.079     Document Type: Article

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