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Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of C-7-Substituted 1,3-Benzothiazole Derivatives

https://doi.org/10.1021/jm400778d
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1 of the 33 references listed on this page is in the Retraction Watch database as retracted (export 2026-11-04): 10.1016/j.dit.2013.03.005 (notice 2013-05-22).

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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

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Arzneimittelsynthetische Studien IV. Synthese schwefelhaltiger Verbindungen
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Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF
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Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial
inferredcites →https://doi.org/10.1016/s1074-5521(99)80088-xopenalex-snapshot
Paradoxical activation of Raf by a novel Raf inhibitor
inferredcites →https://doi.org/10.1021/bi101777fopenalex-snapshot
Biochemical Characterization of TAK-593, a Novel VEGFR/PDGFR Inhibitor with a Two-Step Slow Binding Mechanism
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Small Molecule Conformational Preferences Derived from Crystal Structure Data. A Medicinal Chemistry Focused Analysis
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van der Waals Volumes and Radii
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Derivatives of 2-Amino-6-methoxybenzothiazole
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N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide. A novel, systemically active antitumor agent effective against 3LL Lewis Lung carcinoma
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Design and Synthesis of Novel DFG-Out RAF/Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Inhibitors. 1. Exploration of [5,6]-Fused Bicyclic Scaffolds
inferredcites →https://doi.org/10.1021/jo01299a041openalex-snapshot
Synthesis of benzothiazoles. .alpha.-Amino-(4-hydroxy-6-benzothiazolyl)propionic acid
inferredcites →https://doi.org/10.1038/nature08833openalex-snapshot
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
inferredcites →https://doi.org/10.1038/nature08902openalex-snapshot
RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
inferredcites →https://doi.org/10.1038/nature09454openalex-snapshot
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
inferredcites →https://doi.org/10.1038/nchembio.1257openalex-snapshot
Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization
inferredcites →https://doi.org/10.1038/nrclinonc.2011.69openalex-snapshot
BRAF targeted therapy changes the treatment paradigm in melanoma
inferredcites →https://doi.org/10.1038/nrd2082openalex-snapshot
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inferredcites →https://doi.org/10.1038/onc.2011.160openalex-snapshot
Raf kinases in cancer–roles and therapeutic opportunities
inferredcites →https://doi.org/10.1056/nejmoa1002011openalex-snapshot
Inhibition of Mutated, Activated BRAF in Metastatic Melanoma
inferredcites →https://doi.org/10.1056/nejmoa1103782openalex-snapshot
Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation
inferredcites →https://doi.org/10.1056/nejmoa1105358openalex-snapshot
RAS Mutations in Cutaneous Squamous-Cell Carcinomas in Patients Treated with BRAF Inhibitors
inferredcites →https://doi.org/10.1073/pnas.0711741105openalex-snapshot
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inferredcites →https://doi.org/10.1111/j.1365-2133.2012.11155.xopenalex-snapshot
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inferredcites →https://doi.org/10.1158/0008-5472.can-04-1168openalex-snapshot
A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib)
inferredcites →https://doi.org/10.1158/0008-5472.can-10-0646openalex-snapshot
RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models
inferredcites →https://doi.org/10.1158/1535-7163.mct-10-0181openalex-snapshot
Selective and Potent Raf Inhibitors Paradoxically Stimulate Normal Cell Proliferation and Tumor Growth
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SYNTHESIS OF SOME 5-NITRO-2-FURFURYLIDENE DERIVATIVES AND THEIR ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES
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Crystal Structure of the Kinase domain of Human B-raf with a [1,3]thiazolo[5,4-b]pyridine derivative

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

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Synthesis, molecular modeling and biological evaluation of novel imatinib derivatives as anticancer agents
inferred← citeshttps://doi.org/10.3978/j.issn.2305-5839.2015.08.12openalex-snapshot
Other targeted drugs in melanoma.
inferred← citeshttps://doi.org/10.6084/m9.figshare.26690965openalex-snapshot
Additional file 1 of Construction of luciferase-expressing Neospora caninum and drug screening
inferred← citeshttps://doi.org/10.6084/m9.figshare.26690968openalex-snapshot
Additional file 2 of Construction of luciferase-expressing Neospora caninum and drug screening
inferred← citeshttps://doi.org/10.6084/m9.figshare.26690971openalex-snapshot
Additional file 3 of Construction of luciferase-expressing Neospora caninum and drug screening
inferred← citeshttps://doi.org/10.7150/jca.76695openalex-snapshot
KRAS as a Key Oncogene in the Clinical Precision Diagnosis and Treatment of Pancreatic Cancer
inferred← citeshttps://doi.org/10.7554/elife.95481openalex-snapshot
Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitors
inferred← citeshttps://doi.org/10.7554/elife.95481.1openalex-snapshot
Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitors
inferred← citeshttps://doi.org/10.7554/elife.95481.2openalex-snapshot
Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitors
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