Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177) (English)
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In:
Journal of medicinal chemistry
;
59
, 17
; 7915
;
2016
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ISSN:
- Article (Journal) / Print
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Title:Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177)
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Contributors:De Lucca, George V ( author ) / Shi, Qing / Liu, Qingjie / Batt, Douglas G / Beaudoin Bertrand, Myra / Rampulla, Rick / Mathur, Arvind / Discenza, Lorell / D'Arienzo, Celia / Dai, Jun
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Published in:Journal of medicinal chemistry ; 59, 17 ; 7915
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Publisher:
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Place of publication:Easton, Pa.
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Publication date:2016
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ISSN:
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ZDBID:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
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- Further information on Basic classification
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Keywords:
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Classification:
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Source:
Table of contents – Volume 59, Issue 17
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 7699
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Polymerase Acidic Protein–Basic Protein 1 (PA–PB1) Protein–Protein Interaction as a Target for Next-Generation Anti-influenza TherapeuticsMassari, Serena / Goracci, Laura / Desantis, Jenny / Tabarrini, Oriana et al. | 2016
- 7719
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Notch Antagonists: Potential Modulators of Cancer and Inflammatory DiseasesKumar, Rajesh / Juillerat-Jeanneret, Lucienne / Golshayan, Dela et al. | 2016
- 7738
-
Challenges and Opportunities for the Application of Boron Clusters in Drug DesignLeśnikowski, Zbigniew J. et al. | 2016
- 7759
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From Companion Diagnostics to Theranostics: A New Avenue for Alzheimer’s Disease?Bolognesi, Maria Laura / Gandini, Annachiara / Prati, Federica / Uliassi, Elisa et al. | 2016
- 7771
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Allosteric Modulation of Phosphatase Activity May Redefine Therapeutic ValueSalamoun, Joseph M. / Wipf, Peter et al. | 2016
- 7773
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Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase InhibitorGarcia Fortanet, Jorge / Chen, Christine Hiu-Tung / Chen, Ying-Nan P. / Chen, Zhouliang / Deng, Zhan / Firestone, Brant / Fekkes, Peter / Fodor, Michelle / Fortin, Pascal D. / Fridrich, Cary et al. | 2016
- 7783
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Discovery, Synthesis, and Evaluation of 2,4-Diaminoquinazolines as a Novel Class of Pancreatic β‑Cell-Protective Agents against Endoplasmic Reticulum (ER) StressDuan, Hongliang / Lee, Jae Wook / Moon, Sung Won / Arora, Daleep / Li, Yu / Lim, Hui-Ying / Wang, Weidong et al. | 2016
- 7801
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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)Bradbury, Robert H. / Callis, Rowena / Carr, Gregory R. / Chen, Huawei / Clark, Edwin / Feron, Lyman / Glossop, Steve / Graham, Mark A. / Hattersley, Maureen / Jones, Chris et al. | 2016
- 7818
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Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 InhibitorsDiMauro, Erin F. / Altmann, Stephen / Berry, Loren M. / Bregman, Howard / Chakka, Nagasree / Chu-Moyer, Margaret / Bojic, Elma Feric / Foti, Robert S. / Fremeau, Robert / Gao, Hua et al. | 2016
- 7840
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Development of a High-Affinity PET Radioligand for Imaging Cannabinoid Subtype 2 ReceptorMoldovan, Rareş-Petru / Teodoro, Rodrigo / Gao, Yongjun / Deuther-Conrad, Winnie / Kranz, Mathias / Wang, Yuchuan / Kuwabara, Hiroto / Nakano, Masayoshi / Valentine, Heather / Fischer, Steffen et al. | 2016
- 7856
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Tumor Targeting with Novel 6‑Substituted Pyrrolo [2,3‑d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide BiosynthesisGolani, Lalit K. / Wallace-Povirk, Adrianne / Deis, Siobhan M. / Wong, Jennifer / Ke, Jiyuan / Gu, Xin / Raghavan, Sudhir / Wilson, Mike R. / Li, Xinxin / Polin, Lisa et al. | 2016
- 7877
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Small Antimicrobial Agents Based on Acylated Reduced Amide ScaffoldTeng, Peng / Huo, Da / Nimmagadda, Alekhya / Wu, Jianfeng / She, Fengyu / Su, Ma / Lin, Xiaoyang / Yan, Jiyu / Cao, Annie / Xi, Chuanwu et al. | 2016
- 7888
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Apo- and Antagonist-Binding Structures of Vitamin D Receptor Ligand-Binding Domain Revealed by Hybrid Approach Combining Small-Angle X‑ray Scattering and Molecular DynamicsAnami, Yasuaki / Shimizu, Nobutaka / Ekimoto, Toru / Egawa, Daichi / Itoh, Toshimasa / Ikeguchi, Mitsunori / Yamamoto, Keiko et al. | 2016
- 7901
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Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial HypertensionShaw, Duncan E. / Baig, Ferheen / Bruce, Ian / Chamoin, Sylvie / Collingwood, Stephen P. / Cross, Sarah / Dayal, Satish / Drückes, Peter / Furet, Pascal / Furminger, Vikki et al. | 2016
- 7915
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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7‑(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]‑9H‑carbazole-1-carboxamide (BMS-935177)De Lucca, George V. / Shi, Qing / Liu, Qingjie / Batt, Douglas G. / Beaudoin Bertrand, Myra / Rampulla, Rick / Mathur, Arvind / Discenza, Lorell / D’Arienzo, Celia / Dai, Jun et al. | 2016
- 7936
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Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B VirusMcGowan, David / Herschke, Florence / Pauwels, Frederik / Stoops, Bart / Last, Stefaan / Pieters, Serge / Scholliers, Annick / Thoné, Tine / Van Schoubroeck, Bertrand / De Pooter, Dorien et al. | 2016
- 7950
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Hit-to-Lead Studies for the Antimalarial Tetrahydroisoquinolone CarboxanilidesFloyd, David M. / Stein, Philip / Wang, Zheng / Liu, Jian / Castro, Steve / Clark, Julie A. / Connelly, Michele / Zhu, Fangyi / Holbrook, Gloria / Matheny, Amy et al. | 2016
- 7963
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Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole ArmKlich, Katarzyna / Pyta, Krystian / Kubicka, Marcelina M. / Ruszkowski, Piotr / Celewicz, Lech / Gajecka, Marzena / Przybylski, Piotr et al. | 2016
- 7974
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Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia CellsLiao, Yi / Niu, Xiaojia / Chen, Bailing / Edwards, Holly / Xu, Liping / Xie, Chengzhi / Lin, Hai / Polin, Lisa / Taub, Jeffrey W. / Ge, Yubin et al. | 2016
- 7991
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Design, Synthesis, and Evaluation of Thiophene[3,2‑d]pyrimidine Derivatives as HIV‑1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance ProfilesKang, Dongwei / Fang, Zengjun / Li, Zhenyu / Huang, Boshi / Zhang, Heng / Lu, Xueyi / Xu, Haoran / Zhou, Zhongxia / Ding, Xiao / Daelemans, Dirk et al. | 2016
- 8008
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Effects of 5‑O‑Ribosylation of Aminoglycosides on Antimicrobial Activity and Selective Perturbation of Bacterial TranslationHerzog, Ido M. / Louzoun Zada, Sivan / Fridman, Micha et al. | 2016
- 8019
-
Identification of Inhibitors for the DEDDh Family of Exonucleases and a Unique Inhibition Mechanism by Crystal Structure Analysis of CRN‑4 Bound with 2‑Morpholin-4-ylethanesulfonate (MES)Huang, Kuan-Wei / Hsu, Kai-Cheng / Chu, Lee-Ya / Yang, Jinn-Moon / Yuan, Hanna S. / Hsiao, Yu-Yuan et al. | 2016
- 8030
-
Design, Synthesis, and Bioactivation of O‑Glycosylated Prodrugs of the Natural Nitric Oxide Precursor N ω‑Hydroxy‑l‑arginineLitty, Felix-A. / Gudd, Julia / Girreser, Ulrich / Clement, Bernd / Schade, Dennis et al. | 2016
- 8042
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Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily DosingSun, Li-Qiang / Mull, Eric / Zheng, Barbara / D’Andrea, Stanley / Zhao, Qian / Wang, Alan Xiangdong / Sin, Ny / Venables, Brian L. / Sit, Sing-Yuen / Chen, Yan et al. | 2016
- 8061
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Pyridyl-alanine as a Hydrophilic, Aromatic Element in Peptide Structural OptimizationMroz, Piotr A. / Perez-Tilve, Diego / Liu, Fa / Gelfanov, Vasily / DiMarchi, Richard D. / Mayer, John P. et al. | 2016
- 8068
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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic NephropathyCameron, Kimberly O. / Kung, Daniel W. / Kalgutkar, Amit S. / Kurumbail, Ravi G. / Miller, Russell / Salatto, Christopher T. / Ward, Jessica / Withka, Jane M. / Bhattacharya, Samit K. / Boehm, Markus et al. | 2016
- 8082
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Human Toll-like Receptor (TLR) 8‑Specific Agonistic Activity in Substituted Pyrimidine-2,4-diaminesBeesu, Mallesh / Salyer, Alex C. D. / Trautman, Kathryn L. / Hill, Justin K. / David, Sunil A. et al. | 2016
- 8094
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Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6)Hendrick, Alan G. / Müller, Ilka / Willems, Henriëtte / Leonard, Philip M. / Irving, Steve / Davenport, Richard / Ito, Takashi / Reeves, Jenny / Wright, Susanne / Allen, Vivienne et al. | 2016
- 8103
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Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4‑d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor FamilySmaill, Jeff B. / Gonzales, Andrea J. / Spicer, Julie A. / Lee, Helen / Reed, Jessica E. / Sexton, Karen / Althaus, Irene W. / Zhu, Tong / Black, Shannon L. / Blaser, Adrian et al. | 2016
- 8125
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1,2-Benzisoselenazol-3(2H)‑one Derivatives As a New Class of Bacterial Urease InhibitorsMacegoniuk, Katarzyna / Grela, Ewa / Palus, Jerzy / Rudzińska-Szostak, Ewa / Grabowiecka, Agnieszka / Biernat, Monika / Berlicki, Łukasz et al. | 2016
- 8134
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Fulvestrant‑3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD)Liu, Jiawang / Zheng, Shilong / Akerstrom, Victoria L. / Yuan, Chester / Ma, Youning / Zhong, Qiu / Zhang, Changde / Zhang, Qiang / Guo, Shanchun / Ma, Peng et al. | 2016
- 8141
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A Selective Galactose–Coumarin-Derived Galectin‑3 Inhibitor Demonstrates Involvement of Galectin-3-glycan Interactions in a Pulmonary Fibrosis ModelRajput, Vishal K. / MacKinnon, Alison / Mandal, Santanu / Collins, Patrick / Blanchard, Helen / Leffler, Hakon / Sethi, Tariq / Schambye, Hans / Mukhopadhyay, Balaram / Nilsson, Ulf J. et al. | 2016
- 8148
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Correction to Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory DiseaseAmour, Augustin / Barton, Nick / Cooper, Anthony W. J. / Inglis, Graham / Jamieson, Craig / Luscombe, Christopher N. / Morrell, Josie / Peace, Simon / Perez, David / Rowland, Paul et al. | 2016