Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability (original) (raw)

Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold

Yang Ge

Bioorganic & medicinal chemistry, 2014

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Potent and Selective Bruton’s Tyrosine Kinase Inhibitors: Discovery of GDC-0834

Scott Mitchell

Bioorganic & Medicinal Chemistry Letters, 2015

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Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes

Thierry Fischmann

Bioorganic & Medicinal Chemistry Letters, 2020

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Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors

Zhenquan Hu

European journal of medicinal chemistry, 2017

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Development of a Scalable Synthesis for the Potent Kinase Inhibitor, BMS-986236; 1-(5-(4-(3-hydroxy-3-methylbutyl)-1H-1,2,3-triazol-1-yl)-4-(isopropylamino) pyridin-2-yl)-1H-pyrazolo[3,4-b] pyridine-5-carbonitrile

Anki Reddy

Organic Process Research & Development, 2019

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Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase

Kevin D Jerome, Jeff Hitchcock, Brian Hickory

Bioorganic & Medicinal Chemistry Letters, 2011

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Discovery of 3-[2-(Imidazo[1,2- b ]pyridazin-3-yl)ethynyl]-4-methyl- N -{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

Xiaotian Zhu, Raji Sundaramoorthi

Journal of Medicinal Chemistry, 2010

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Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization

Michael Kubbutat

Bioorganic & Medicinal Chemistry, 2009

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Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors

Steven Kim

Bioorganic & Medicinal Chemistry Letters, 2009

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Design, synthesis, anticancer evaluation and molecular docking of new V600EBRAF inhibitors derived from pyridopyrazinone

Prof. Mandava venkata Basaveswara Rao

European Journal of Chemistry, 2016

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The pyrazolobenzothiazine core as a new chemotype of p38 alpha mitogen-activated protein kinase inhibitors

Maria Letizia Barreca

Chemical biology & drug design, 2015

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Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation

Juan Espinosa

Bioorganic & medicinal chemistry letters, 2004

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Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor

Zhenquan Hu

European journal of medicinal chemistry, 2017

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p38 MAP kinase inhibitors. Part 6: 2-Arylpyridazin-3-ones as templates for inhibitor design

Giovanna Scapin

Bioorganic & Medicinal Chemistry Letters, 2006

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Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors

Claire Delehouze

European journal of medicinal chemistry, 2016

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The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines

Juan Manuel Real Espinosa

Molecular Cancer Therapeutics, 2004

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Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors

Gerald Shipps

Bioorganic & Medicinal Chemistry Letters, 2011

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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

Adam Johnson

ACS medicinal chemistry letters, 2017

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Discovery of novel BTK inhibitors with carboxylic acids

Thierry Fischmann

Bioorganic & Medicinal Chemistry Letters, 2017

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Synthesis and biological evaluation of 3,6-diamino-1 H-pyrazolo[3,4- b]pyridine derivatives as protein kinase inhibitors

Abdelouahid Samadi

Bioorganic & Medicinal Chemistry Letters, 19 (16), 4566-4569, 2009 , 2009

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Discovery and Evaluation of 7-Alkyl-1,5-bis-aryl-pyrazolopyridinones as Highly Potent, Selective, and Orally Efficacious Inhibitors of p38α Mitogen-Activated Protein Kinase ⊥ ⊥ Atomic coordinates and structure factors for crystal structure of compound 3d with p38α can be accessed using PDB code 3LHJ

Helen McBride, Ryan Wurz

Journal of Medicinal Chemistry, 2010

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Ethyl 2-(benzylidene)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylate analogues as a new scaffold for protein kinase casein kinase 2 inhibitor

Kyu-Yeon Jun

Bioorganic & medicinal chemistry, 2014

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Structural and atropisomeric factors governing the selectivity of pyrimido-benzodiazipinones as inhibitors of kinases and bromodomains

Jose Miguel Lizcano

ACS chemical biology, 2018

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