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Results for “Pyridine”
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Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 I
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Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exp
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Discovery of ( S )-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1 H -pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1 H )-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development
The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream nodes with RAF and MEK inhibitors has proven effective clinically, resistance frequently develops through reactivation of the pathway. Simultaneous targeting of multiple nodes in the pathway, such as MEK and ERK, offers the prospect of enhanced efficacy as well as reduced potential for acquired resistance. Here, described herein is the discovery and characterization of GDC-0994 (22), an orally bioavailable small molecule inhibitor selective for ERK kinase activity.
1,2,4-Triazolo-[1,5- a ]Pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors with a Novel Monodentate Binding Interaction
Abstract not provided
Discovery of Potent, Selective, and Brain-Penetrant 1H-Pyrazol-5-yl-1H-pyrrolo[2,3-b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors
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Boron Dipyridylmethene (DIPYR) Dyes: Shedding Light on Pyridine-Based Chromophores
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Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5- d ]pyrrolo[2,3- b ]pyridine Inhibitors
Early hit to lead work on a pyrrolopyridine chemotype provided access to compounds with biochemical and cellular potency against Janus kinase 2 (JAK2). Structure-based drug design along the extended hinge region of JAK2 led to the identification of an important H-bond interaction with the side chain of Tyr 931, which improved JAK family selectivity. The 4,5-dimethyl thiazole analogue 18 demonstrated high levels of JAK family selectivity and was identified as a promising lead for the program.
Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2
Abstract not provided
Discovery of Pyridazinone and Pyrazolo[1,5- a ]pyridine Inhibitors of C-Terminal Src Kinase
Abstract not provided
Crystal Growth, Single Crystal Structure, and Biological Activity of Thiazolo-Pyridine Dicarboxylic Acid Derivatives
Four novel TPDCA derivatives were prepared via a supersaturation method combining TPDCA with water, N-methyl-2-pyrrolidone (NMP), Na(PO 2 H 2 ), and ammonia solution: 2(C 9 H 7 NO 5 S)H 2 O (1), (C 9 H 7 NO 5 S)C 5 H 9 NO (2), (C 9 H 7 NO 5 S)Na(PO 2 H 2 ) (3), and (C 9 H 5 NO 5 S)(NH 4 )2(H 2 O) (4). Their crystal structures were determined by single-crystal X-ray diffraction. Compounds (1) and (2) crystallize in the monoclinic space groups P2 1 and P2 1 /c, respectively, whereas compounds (3) and (4) crystallize in the triclinic space group P1 - . Weak and moderate hydrogen bonds were detected in the four compounds. In the biological tests, (1) and (3) exhibited significant antibacterial activity against Escherichia coli and Staphylococcus aureus; in addition, (1) was cytotoxic against leukemia HL-60 cells with the IC 50 value of 158.5 ± 12.5 μM.
Synthesis of Tridentate [1,2,4] Triazinyl-Pyridin-2-yl Indole Lewis Basic Complexants via Pd-Catalyzed Suzuki–Miyaura Cross-Coupling
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