- Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy
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We synthesized a library of aminopyrazole analogs to systematically explore the hydrophobic pocket adjacent to the hinge region and the solvent exposed region of cyclin dependent kinases. Structure-activity relationship studies identified an optimal substitution for the hydrophobic pocket and analog 24 as a potent and selective CDK2/5 inhibitor.
- Rana, Sandeep,Sonawane, Yogesh A.,Taylor, Margaret A.,Kizhake, Smitha,Zahid, Muhammad,Natarajan, Amarnath
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supporting information
p. 3736 - 3740
(2018/10/24)
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- ADENOSINE A3 RECEPTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein is a method of preventing, treating, or ameliorating one or more symptoms of an adenosine A3-mediated condition, disorder, or disease, with a compound of Formula I. Also provided herein is a method of preventing, treating, or ameliorating one or more symptoms of glaucoma or ocular hypertension. Further provided herein is a method of modulating the activity of an adenosine A3 receptor.
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- Rapid reduction of heteroaromatic nitro groups using catalytic transfer hydrogenation with microwave heating
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A method for the rapid, safe reduction of heteroaromatic and aromatic nitro groups to amines is described using catalytic transfer hydrogenation under microwave heating conditions. Commonly available Pd/C or Pt/C catalyst is extremely effective with 1,4-cyclohexadiene as the hydrogen transfer source. In the case of substrates containing potentially labile aromatic halogens, Pt/C is effective and results in little or no dehalogenation. In general, the reactions are complete within 5 min at 120 °C.
- Quinn, John F.,Bryant, Cole E.,Golden, Kathryn C.,Gregg, Brian T.
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experimental part
p. 786 - 789
(2010/03/24)
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- Heterocyclic dihydropyrimidine compounds
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Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
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- Methods of treating cytokine mediated diseases
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Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.
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- Aromatic heterocyclic compounds as antiinflammatory agents
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Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
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- 3-(heteroarylamino)methylene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors
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The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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- Aminopyrazoles. IV. Pyrazol-3- and 5-amines from 2,3-dihaloalkanenitriles or 3-Chloroacrylonitriles and Hydrazines
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2,3-Dihalopropanenitriles and substituted 3-chloropropenenitriles react with hydrazines in basic solution to form either pyrazol-3-amines 4 or pyrazol-5-amines 5 or a mixture of both isomers.
- Ege, Guenter,Franz, Hermann
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p. 1267 - 1273
(2007/10/02)
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