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Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 I

Journal Article · · J. Med. Chem.

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; NCI; NIH
OSTI ID:
1784971
Journal Information:
J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (9) Vol. 64
Country of Publication:
United States
Language:
ENGLISH

References (41)

Microwave-assisted Synthesis of a 3-Aminoimidazo[1,2-a]-pyridine/pyrazine Library by Fluorous Multicomponent Reactions and Subsequent Cross-coupling Reactions journal December 2004
BindingDB in 2015: A public database for medicinal chemistry, computational chemistry and systems pharmacology journal October 2015
Current development of CBP/p300 inhibitors in the last decade journal January 2021
A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation-π Interaction journal May 2014
A Bead-Based Proximity Assay for BRD4 Ligand Discovery: Proximity Assay for BRD4 Ligand Discovery journal November 2015
Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains journal June 2014
Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family journal March 2012
Using Chemical Epigenetics to Target Cancer journal June 2020
Features and development of Coot journal March 2010
Integration, scaling, space-group assignment and post-refinement journal January 2010
Clinical progress and pharmacology of small molecule bromodomain inhibitors journal August 2016
Parallel synthesis of 3-aminoimidazo[1,2-a]pyridines and pyrazines by a new three-component condensation journal May 1998
Open access chemical probes for epigenetic targets journal September 2015
Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology journal September 2016
Bromodomains: a new target class for drug development journal July 2019
Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites journal July 2012
Protein Lysine Acetylation by p300/CBP journal October 2014
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain journal May 2017
Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762 journal January 2014
Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions journal September 2012
Structural Mechanism of the Bromodomain of the Coactivator CBP in p53 Transcriptional Activation journal January 2004
Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities journal December 2015
A New Heterocyclic Multicomponent Reaction For the Combinatorial Synthesis of Fused 3-Aminoimidazoles journal September 1998
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300 journal September 2016
Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A) journal April 2012
A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes journal April 2011
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) journal September 2017
Synthesis of Imidazo[1,2-a] annulated Pyridines, Pyrazines and Pyrimidines by a Novel Three-Component Condensation journal June 1998
Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors journal October 2014
The epigenetic regulators CBP and p300 facilitate leukemogenesis and represent therapeutic targets in acute myeloid leukemia journal April 2015
Structural Insights into Acetylated-Histone H4 Recognition by the Bromodomain-PHD Finger Module of Human Transcriptional Coactivator CBP journal February 2014
Advancements in the Development of non‐BET Bromodomain Chemical Probes journal January 2019
phenix.model_vs_data : a high-level tool for the calculation of crystallographic model and data statistics journal May 2010
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors journal September 2016
Targeting bromodomains: epigenetic readers of lysine acetylation journal April 2014
CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation journal January 2017
Four domains of p300 each bind tightly to a sequence spanning both transactivation subdomains of p53 journal April 2007
Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition journal June 2016
The Bromodomain: A New Target in Emerging Epigenetic Medicine journal December 2015
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637) journal March 2016
Cross-Coupling Reactions Of Organoboranes: An Easy Way To Construct CC Bonds (Nobel Lecture) journal May 2011

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