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Polo-like kinase 1 (Plk1) is a validated target for the treatment of cancer. In this report, by analyzing amino acid residue differences among the ATP-binding pockets of Plk1, Plk2 and Plk3, novel selective Plk1 inhibitors were designed based on BI 2536 and BI 6727, two Plk1 inhibitors in clinical studies for cancer treatments. The Plk1 inhibitors reported herein have more potent inhibition against Plk1 and better isoform selectivity in the Plk family than these two lead compounds. In addition, by introducing a hydroxyl group, our compounds have significantly improved solubility and may target specific polar residues Arg57, Glu69 and Arg134 of Plk1. Moreover, most of our compounds exhibited antitumor activities in the nanomolar range against several cancer cell lines in the MTT assay. Through this structure-based design strategy and SAR study, a few promising selective Plk1 inhibitors having the tetrahydropteridin scaffold, for example, L34, were identified and could be for further anticancer research.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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High selectivity and yield from aryl-aryl coupling reactions between chlorine-containing aromatic bromides and organoboron reagents are reported. The variable reaction selectivity between the bromine and chlorine mainly depends on the electronic effects of the aromatic substrates. The reactivity of the chlorine can be completely restrained by employing the optimized Palladium catalysts, which can be used for the preparation of the chlorine-bearing molecules. Then, a series of high molecular weight conjugated copolymers with chlorine on the backbones are straight forward synthesized for the first time under Suzuki condensation reaction. The polymers show large Stokes shifts and low self-absorption. Efficient and high brightness red emission centre at about 636 nm can be obtained when doping the resulting polymer into F8BT.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Palladium catalyzed Suzuki-Miyaura cross-coupling reactions are reported for the synthesis of monoarylated (at the C8 position) and symmetrical diarylated (at the C6 and C8 positions) imidazo[1,2-a]pyrazines. Monoarylated products have also been used to synthesize unsymmetrical C6/C8 diarylated products. These compounds were screened for in vitro antitumor activities against a preliminary tumor cell line panel assay.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A blue fluorescent compound includes a host material being capable of transporting an electron or a hole; and a dopant material represented by following Formula 1: wherein at least two of the R1, the R2, the R3, and the R4 are selected from substituted or non-substituted aromatic group or substituted or non-substituted heterocyclic group, and the R5 is selected from substituted or non-substituted aromatic group or substituted or non-substituted heterocyclic group.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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In this communication, we developed a new procedure for the direct carbonylative transformation of benzyl amines. Using dimethyl carbonate as the solvent, methyl 2-arylacetates can be produced in good to excellent yields from the corresponding primary, secondary, and tertiary benzyl amines with palladium as the catalyst. Notably, no base or any other additive is required here. In addition, our procedure can also be applied in the preparation of methylphenidate, which is a marketing drug and used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The present invention discloses a kind of naphthalene and furan structure Biaryl Monophosphine ligand and its preparation method and application, the biaryl Monophosphine ligand shown in formula (VIII) is a compound of chemical formula or its enantiomer or racemate. Biaryl Monophosphine ligand of this invention by introducing the furan ring, and the binaphthyl forming conjugated structure, the metallisation is increased, including its enantiomer or racemate the steric hindrance of the electron cloud density and its aromatic ring, improve the stability of the complex, and adjusting the ligand with sterically hindered, ligand novel structure, Sonogashira reaction of the preparation process, ring in the molecule, such as C-P coupling reaction, the synthetic method is simple, the resulting biligand applied to reaction Suzuki-Miyuara has high activity, selectivity, and the like. (by machine translation)

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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We report the synthesis of a series of A1?pi?A2?pi?A1-type small molecules, DPP2T-RH, DPPFT-RH, and DPPT-RH, in which thiophene and furan were introduced to bridge the two strong electron-withdrawing units of DPP and rhodanine (RH). Interestingly, these DPP-RH-based small molecules exhibited ambipolar characteristics, showing photovoltaic performance both as donors and acceptors in combination with PC71BM and P3HT, respectively. The best power conversion efficiencies were obtained from DPPFT-RH (1.77%) and DPP2T-RH (1.28%) as donor and acceptor, respectively. Their physical properties, film packing ability, and photovoltaic performances were fine-tuned by rational design of the pi-bridges.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Diversity-oriented synthesis of fused tetracyclic 6,11- dihydroquinoxalino[2,3-b]quinolines is described via a sequential Ugi-variant multicomponent reaction and Pd-catalyzed bis-annulation in one-pot process.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method