The discovery of macrocyclic XIAP antagonists from a DNA-programmed chemistry library, and their optimization to give lead compounds with in vivo antitumor activity

Journal of Medicinal Chemistry

Volumn 58, Issue 6, 2015, Pages 2855-2861

  Seigal, Benjamin A ^a   Connors, William H ^a   Fraley, Andrew ^a   Borzilleri, Robert M ^b   Carter, Percy H ^b   Emanuel, Stuart L ^b   Fargnoli, Joseph ^b   Kim, Kyoung ^b   Lei, Ming ^b   Naglich, Joseph G ^b   Pokross, Matthew E ^b   Posy, Shana L ^b   Shen, Henry ^b   Surti, Neha ^b   Talbott, Randy ^b   Zhang, Yong ^b   Terrett, Nicholas K ^a  

^a Ensemble Therapeutics Corp   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; BIR2 PROTEIN; BIR3 PROTEIN; CASPASE 3; MACROCYCLIC COMPOUND; UNCLASSIFIED DRUG; X LINKED INHIBITOR OF APOPTOSIS; X LINKED INHIBITOR OF APOPTOSIS INHIBITOR;

ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BREAST CANCER; CRYSTAL STRUCTURE; DNA LIBRARY; DNA TEMPLATE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; IN VIVO STUDY; MELANOMA; MOUSE; NONHUMAN; TUMOR XENOGRAFT; ANIMAL; ANTAGONISTS AND INHIBITORS; BREAST; BREAST NEOPLASMS; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; FEMALE; GENE LIBRARY; METABOLISM; PATHOLOGY; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTINEOPLASTIC AGENTS; BREAST; BREAST NEOPLASMS; CASPASE 3; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; FEMALE; GENE LIBRARY; HUMANS; MACROCYCLIC COMPOUNDS; MICE; MODELS, MOLECULAR; X-LINKED INHIBITOR OF APOPTOSIS PROTEIN;

EID: 84925935866     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501892g     Document Type: Article

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