Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate
出版年份 2022 全文链接
标题
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate
作者
关键词
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出版物
JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue 3, Pages 2262-2287
出版商
American Chemical Society (ACS)
发表日期
2022-01-08
DOI
10.1021/acs.jmedchem.1c01747
参考文献
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注意:仅列出部分参考文献,下载原文获取全部文献信息。- Achieving clinical success with BET inhibitors as anti-cancer agents
- (2021) Tatiana Shorstova et al. BRITISH JOURNAL OF CANCER
- Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design
- (2021) Ashvinikumar V. Gavai et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression
- (2021) Katherine L. Jones et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening
- (2020) Christopher R. Wellaway et al. JOURNAL OF MEDICINAL CHEMISTRY
- Understanding Idiosyncratic Toxicity: Lessons Learned from Drug-Induced Liver Injury
- (2020) Merrie Mosedale et al. JOURNAL OF MEDICINAL CHEMISTRY
- Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer
- (2020) Emily J. Faivre et al. NATURE
- Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
- (2020) George S. Sheppard et al. JOURNAL OF MEDICINAL CHEMISTRY
- Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation
- (2020) Omer Gilan et al. SCIENCE
- The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins
- (2020) Alex Preston et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
- (2020) Jonathan Thomas Seal et al. JOURNAL OF MEDICINAL CHEMISTRY
- GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins
- (2020) Robert J. Watson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
- (2020) Christopher R. Wellaway et al. JOURNAL OF MEDICINAL CHEMISTRY
- An Adaptive Physiologically Based Pharmacokinetic–Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers
- (2020) Kylie Riddell et al. JOURNAL OF CLINICAL PHARMACOLOGY
- Advancements in the Development of non-BET Bromodomain Chemical Probes
- (2019) Michael A. Clegg et al. ChemMedChem
- First-in-human phase I study of the bromodomain and extraterminal motif inhibitor BAY 1238097: emerging pharmacokinetic/pharmacodynamic relationship and early termination due to unexpected toxicity
- (2019) Sophie Postel-Vinay et al. EUROPEAN JOURNAL OF CANCER
- Fraction Unbound for Liver Microsome and Hepatocyte Incubations for All Major Species Can Be Approximated Using a Single-Species Surrogate
- (2019) John T. Barr et al. DRUG METABOLISM AND DISPOSITION
- Bromodomain biology and drug discovery
- (2019) Nilesh Zaware et al. NATURE STRUCTURAL & MOLECULAR BIOLOGY
- Disrupting Acetyl-lysine Interactions: Recent Advance in the Development of BET Inhibitors
- (2018) Fa Zhang et al. CURRENT DRUG TARGETS
- Lipophilic Efficiency as an Important Metric in Drug Design
- (2018) Ted W. Johnson et al. JOURNAL OF MEDICINAL CHEMISTRY
- BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor
- (2018) Hatice Gulcin Ozer et al. Cancer Discovery
- Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
- (2017) Keith F. McDaniel et al. JOURNAL OF MEDICINAL CHEMISTRY
- Bromodomain Histone Readers and Cancer
- (2017) Abhinav K Jain et al. JOURNAL OF MOLECULAR BIOLOGY
- Quality guidelines for oral drug candidates: dose, solubility and lipophilicity
- (2016) Martin K. Bayliss et al. DRUG DISCOVERY TODAY
- Bromodomain and extra-terminal (BET) family proteins: New therapeutic targets in major diseases
- (2016) Balasundaram Padmanabhan et al. JOURNAL OF BIOSCIENCES
- Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)
- (2016) Robert H. Bradbury et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials
- (2016) Brian K. Albrecht et al. JOURNAL OF MEDICINAL CHEMISTRY
- Potent and selective bivalent inhibitors of BET bromodomains
- (2016) Michael J Waring et al. Nature Chemical Biology
- The Bromodomain: A New Target in Emerging Epigenetic Medicine
- (2015) Steven G. Smith et al. ACS Chemical Biology
- Abstract 3523: Discovery of a novel BET inhibitor INCB054329
- (2015) Phillip CC Liu et al. CANCER RESEARCH
- Abstract CT231: BET-bromodomain inhibitor OTX015 shows clinically meaningful activity at nontoxic doses: interim results of an ongoing phase I trial in hematologic malignancies
- (2015) Patrice E. Herait et al. CANCER RESEARCH
- The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor
- (2014) Romain Gosmini et al. JOURNAL OF MEDICINAL CHEMISTRY
- Targeting bromodomains: epigenetic readers of lysine acetylation
- (2014) Panagis Filippakopoulos et al. NATURE REVIEWS DRUG DISCOVERY
- Lipophilic efficiency: the most important efficiency metric in medicinal chemistry
- (2013) Kevin D Freeman-Cook et al. Future Medicinal Chemistry
- Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
- (2013) Olivier Mirguet et al. JOURNAL OF MEDICINAL CHEMISTRY
- Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
- (2013) David S. Hewings et al. JOURNAL OF MEDICINAL CHEMISTRY
- From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151
- (2012) Olivier Mirguet et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Clinicopathologic Features and Long-term Outcomes of NUT Midline Carcinoma
- (2012) D. E. Bauer et al. CLINICAL CANCER RESEARCH
- Bromodomains as therapeutic targets
- (2011) Susanne Muller et al. EXPERT REVIEWS IN MOLECULAR MEDICINE
- Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery
- (2011) Chun-wa Chung et al. JOURNAL OF MEDICINAL CHEMISTRY
- Suppression of inflammation by a synthetic histone mimic
- (2010) Edwige Nicodeme et al. NATURE
- Selective inhibition of BET bromodomains
- (2010) Panagis Filippakopoulos et al. NATURE
- Strategic Use of Plasma and Microsome Binding To Exploit in Vitro Clearance in Early Drug Discovery
- (2010) George Chang et al. ACS Medicinal Chemistry Letters
- Chiral Brønsted Acid-Catalyzed Enantioselective Three-Component Povarov Reaction
- (2009) Hua Liu et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Generation of a Set of Simple, Interpretable ADMET Rules of Thumb
- (2008) M. Paul Gleeson JOURNAL OF MEDICINAL CHEMISTRY
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