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9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.
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Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations.
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Small molecule recognition of c-Src via the Imatinib-binding conformation.
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SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib.
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Flying under the radar: the new wave of BCR-ABL inhibitors.
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Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358.
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Ba/F3 cells and their use in kinase drug discovery.
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In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells.
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N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
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A general strategy for creating "inactive-conformation" abl inhibitors.
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