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The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N64 – PubChem

 

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Compounds and compositions are presented that inhibit K-ras, and especially mutant K-ras. Certain compounds preferentially or even selectively inhibit specific forms of mutant K-Ras, and particularly the G12D mutant form.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N40 – PubChem

 

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Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.Read on for other articles about 5469-70-5Electric Literature of 5469-70-5

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Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N35 – PubChem

 

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The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules.Read on for other articles about 5469-70-5Electric Literature of 5469-70-5

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The invention relates to a process for relaxing keratin fibres by applying to the keratin fibres a relaxing composition containing at least one denaturing agent with a molecular mass of greater than 18.1 g/mol, present in a molar concentration of between 1M and 8M, and raising the temperature of the keratin fibres to a temperature of between 110 and 250 C.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N50 – PubChem

 

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Modeling chemical reactions helps engineers virtually understand the chemistry, optimal size and design of the system, and how it interacts with other physics that may come into play. Safety of 3-Aminopyridazine

(Figure Presented) CuI/L5 (N,N?-dimethylethylenediamine) proves to be an efficient catalyst system for the amination of arylhalides with guanidines. The same catalyst system is then successfully applied to the one-step synthesis of 1-H-2-aminobenzimidazoles through tandem aminations of 1,2-dihaloarenes in modest yields. This methodology is also applicable for the preparation of 1-H or 1-substutituted 2-aryl- or 2-alkyl-benzimidazoles.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N70 – PubChem

 

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Focusing on the marine-derived alkaloid ageladine A ([4-(4,5-dibromo-1H-pyrrol-2-yl)]-1H-imidazo[4,5-c]pyridin-2-amine trifluoroacetate), we combined and modified published strategies to develop a synthesis method with easily managed reaction steps that allows gram-scale batch synthesis. On exploration additional features of the fluorescent properties of the compound were revealed. In tissues and cells of a marine flatworm, the emission profile shifted to longer wavelengths than in water. The fluorescence emission maximum shifted around 30-450 nm and the profile showed sufficient intensity at approximately 550 nm and above.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N84 – PubChem

 

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Monomeric and polymeric organosilicon derivatives of 1-acetylguanidine, which exhibits sorption properties, were synthesized. The organosilicon polymers prepared were studied as sorbents for heavy [Hg(II)] and noble [Ag(I), Au(III), Rh(III), Pd(II), Pt(IV)] metals. They actively take up platinum group metals and exhibit metallochromic properties by analogy with the starting compound, 1-acetylguanidine. Their interaction with all the elements studied is accompanied by coloration. The initial monomers exhibit similar metallochromic properties.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N86 – PubChem

 

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Synthetic methodology studies are reported towards the preparation of new propargylic ketones with CF2R side chains. These molecules are used for the synthesis of various types of five- or six-membered heterocycles with difluoroalkyl side chains.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N59 – PubChem

 

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The first total synthesis of the biologically significant bis-indole alkaloid dragmacidin D (5) has been achieved. Thermal and electronic modulation provides the key for a series of palladium-catalyzed Suzuki cross-coupling reactions that furnished the core structure of the complex guanidine- and aminoimidazole-containing dragmacidins. Following this crucial sequence, a succession of meticulously controlled final events was developed leading to the completion of the natural product.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N72 – PubChem

 

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A number of novel amidine containing heterocycles were designed to reproduce the unique interaction pattern, revealed by X-ray crystallography, between the BACE-1 catalytic diad and a weak NMR screening hit (3), with special attention paid to maintaining the appropriate basicity and limiting the number of H-bonding donors of these scaffolds. The iminohydantoin cores (10 and 23) were examined first and found to interact with the catalytic diad in one of two binding modes (A and B), each with the iminohydantoin core flipped 180 in relation to the other. The amidine structural motif within each core forms a bidentate interaction with a different aspartic acid of the catalytic diad. Both modes reproduced a highly conserved interaction pattern between the inhibitors and the catalytic aspartates, as revealed by 3. Potent iminohydantoin BACE-1 inhibitors have been obtained, validating the molecular design as aspartyl protease catalytic site inhibitors. Brain penetrant small molecule BACE inhibitors with high ligand efficiencies have been discovered, enabling multiple strategies for further development of these inhibitors into highly potent, selective and in vivo efficacious BACE inhibitors.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N103 – PubChem