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The study of new dipolar A-pi-D molecules, which have an acceptor (A) and donor (D) charge joined by a conjugate bridge, have been an attention focus in the recent years due their different properties. In the current work, a molecular system has been modified in order to compare the effect on properties, such as quantum yield. Thus, two series were generated (alkyl- and alkoxy-substituted) to determine if molecules with tertiary asymmetric amines change their optical properties and whether quantum yield is affected. The different products have been characterized by several techniques such as UV?Vis spectrophotometry, elemental analysis, NMR, FT-IR, mass spectroscopy and fluorescence spectroscopy. Furthermore, their behavior in eight organic solvents, dichloromethane, tetrahydrofuran, ethyl acetate, 1,4-dioxane, acetone, acetonitrile, dimethylformamide and dimethylsulfoxide were experimentally and theoretically studied. The quantum yields were higher for the alkyl-substituted series. Theoretically, the dihedral angles formed between the tertiary amine and carbonyl group moieties have a correlation with quantum yield values, helping to explain why they are higher in non-polar solvents. Consequently, the maximum quantum yield was obtained with (E)-2-cyano-3-(5-((E)-2-(9,9-diethyl-7-(methyl(phenyl)amino)-9H-fluoren-2-yl) vinyl)thiophen-2-yl)acrylic acid (M8-1) in 1,4-dioxane, reaching 98.8%.

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Four novel functional conjugated tetraarylamines containing a tetraphenylenecore were synthesized via Ni-catalyzed aryl amination followed by McMurry olefination. Their electrochemical properties were studied by cyclic voltammetry, coulometry, and electrolysis monitored by UV-vis spectroscopy, and discussed with regard to those of the known tetrakis(dimethylaminophenyl)ethane.

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An efficient synthetic method for 2-ethoxy-2-oxophosphorindolines, benzo-gamma-phospholactams, has been successfully achieved through the copper-catalyzed intramolecular aromatic C-H insertion of diazophosphonamidates with up to 97% yield. The current method has advantages of mild and clean conditions, and an inexpensive catalyst.

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The important physiological function of microtubules makes them an indispensable and clinically effective target of anti-tumor agents. Herein, we sought to design, synthesize, and evaluate a novel 4-anilinoquinazoline derivative and identify its anti-tumor activity in vitro and in vivo. The novel compound, N-(4-methoxyphenyl)-N-methyl-2-(methyl-d3)quinazolin-4-amine (AQ-4), was identified as a representative scaffold and potent microtubule-targeting agent. As a promising antimitotic agent, AQ-4 displayed remarkable anti-tumor activity with an average IC50 value of 19 nM across a panel of 14 human cancer cell lines. AQ-4 also exhibited nearly identical potent activities against drug-resistant cells, with no evidence of toxicity towards normal cells. A further target verification study revealed that AQ-4 targets the tubulin-microtubule system by significantly inhibiting tubulin polymerization and disrupting the intracellular microtubule spindle dynamics. According to the results of mechanism study, AQ-4 induced cell cycle arrest in the G2/M phase, promoting evident apoptosis and a collapses of mitochondrial membrane potential. The superior anti-tumor effect of AQ-4 in vivo suggests that it should be further investigated to validate its use for cancer therapy.

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The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.

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The present invention is [a], and/or superior EP300 inhibitory activity of the compound or its pharmacologically acceptable salt having a histone acetyltransferase CREBBP there. (1) A compound or pharmacologically acceptable represented by the formula [a] or a salt. [1 A](Wherein, Q (1) of the ring of formula1 , Q ring2 , Q ring3 , X, L and is, each being as defined herein. )[Drawing] no (by machine translation)

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The first examples of titanium-catalyzed hydroaminoalkylation reactions of ethylene with secondary amines are presented. The reactions can be achieved with various titanium catalysts and they do not require the use of high pressure equipment. In addition, the first solid-state structure of a titanapyrrolidine that is formed by insertion of an alkene into the Ti?C bond of a titanaaziridine is reported.

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The electrochemical synthesis of N, N?-disubstituted benzimidazolones from ureas through an intramolecular anodic dehydrogenative N?H/C?H coupling has been developed. The reaction undergoes under the undivided electrolysis conditions and obviates the need for any catalysts and chemical oxidants. (Figure presented.).

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The present invention discloses substituted pyrimidine and pyrimido indole compounds and optionally pharmaceutically acceptable salts, hydrates or solvates thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.

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The present invention is [a], and/or superior EP300 inhibitory activity of the compound or its pharmacologically acceptable salt having a histone acetyltransferase CREBBP there. (1) A compound or pharmacologically acceptable represented by the formula [a] or a salt. [1 A](Wherein, Q (1) of the ring of formula1 , Q ring2 , Q ring3 , X, L and is, each being as defined herein. )[Drawing] no (by machine translation)

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Isoxazole – Wikipedia,
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