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PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. (I)

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Utilizing Mor-DalPhos/palladium-catalyzed monoarylation in the multicomponent one-pot synthesis of indoles

The application of a Mor-DalPhos/palladium catalyst system in the one-pot, multicomponent assembly of substituted indoles from ortho-chlorohaloarenes, alkyl ketones (including acetone), and primary amines is reported. The described protocols offer improved substrate scope in all three reaction components, under more mild conditions and without the need for an additional drying agent. Also reported are the first examples of such multicomponent reactions where all reactants are combined at the start of the reaction, without the need for inert atmosphere reaction conditions.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A iron catalyzed cross-coupling reaction for the dehydrogenation of specification meeting National etherally method (by machine translation)

The invention discloses a iron catalyzed cross-coupling reaction for the dehydrogenation of specification meeting National etherally method, which belongs to the technical field of catalytic synthesis, the reaction formula is as follows: The invention non-toxic inexpensive for the iron does catalyst, silicon reagent as the accelerator, the oxidizing agent under the effect of the cross-coupling reaction for the dehydrogenation of specification meeting National synthetic ether. The invention using environment-friendly iron catalyst, safe and pollution-free silicon reagent promoters, in the dehydrogenation of specification meeting National cross-coupling reaction, has good functional group compatibility, substrate and wide range of application. (by machine translation)

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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PURINE DERIVATIVES USEFUL AS HSP90 INHIBITORS

The present application provides substituted purine derivatives and related compounds of the formulas shown. These compounds are useful as inhibitors of HSP90, and hence in the treatment of related diseases. (Formulae) Z1-Z3 , Xa-Xc, X2 , 324, Y and R are as defined in the specification

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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DDQ-mediated Direct C(sp3)-H Cyanation of Benzyl Ethers and 1,3-Diarylpropenes under Solvent- and Metal-free Conditions

A direct cyanation of benzyl ethers and 1,3-diarylpropenes with TMSCN was performed under solvent- and metal-free conditions. This oxidative cross dehydrative coupling (CDC) reaction was promoted by 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and provided rapid access to a broad range of nitriles in good to excellent yields.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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6-CYCLOPROPYL- AND 6-(1-METHYLCYCLOPROPYL)-1,4-BENZODIOXANES: SYNTHESIS AND NITRATION. REARRANGEMENT OF NITRO SUBSTITUTED 6-CYCLOPROPYL-1,4-BENZODIOXANES USING CONCENTRATED SULFURIC ACID

6-Cyclopropyl- and 6-(1-methylcyclopropyl)-1,4-benzodioxanes have been synthesized as the first cyclopropyl-1,4-benzodioxanes.It was shown that nitration of these compounds occurs with retention of the three carbon ring.In contrast to simple ethers of cyclopropylphenols, nitration leads only to 7-nitro-6-cyclopropyl- and 7-nitro-6-(1-methylcyclopropyl)-1,4-benzodioxanes, respectively.Nitration of 7-nitro-6-cyclopropyl-1,4-benzodioxane occurs regioselectively to give exclusively the 7,8-dinitro product.The structure of the nitration products was confirmed by their rearrangement to the corresponding nitrosopropionyl-1,4-benzodioxanes.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome Chemistry Experiments For 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone

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Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase

Human 5-lipoxygenase (5-LOX) is a well-validated drug target and its inhibitors are potential drugs for treating leukotriene-related disorders. Our previous work on structural optimization of the hit compound 2 from our in-house collection identified two lead compounds, 3a and 3b, exhibiting a potent inhibitory profile against 5-LOX with IC50 values less than 1 mumol/L in cell-based assays. Here, we further optimized these compounds to prepare a class of novel pyrazole derivatives by opening the fused-ring system. Several new compounds exhibited more potent inhibitory activity than the lead compounds against 5-LOX. In particular, compound 4e not only suppressed lipopolysaccharide-induced inflammation in brain inflammatory cells and protected neurons from oxidative toxicity, but also significantly decreased infarct damage in a mouse model of cerebral ischemia. Molecular docking analysis further confirmed the consistency of our theoretical results and experimental data. In conclusion, the excellent in vitro and in vivo inhibitory activities of these compounds against 5-LOX suggested that these novel chemical structures have a promising therapeutic potential to treat leukotriene-related disorders.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The important role of 10288-72-9

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MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for the modulation of elF2B, for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Antiproliferative, antiandrogenic and cytotoxic effects of novel caffeic acid derivatives in LNCaP human androgen-dependent prostate cancer cells

Caffeic acid and its naturally occurring derivative caffeic acid phenethyl ester (CAPE) have antiproliferative and cytotoxic properties in a variety of cancer cell lines without displaying significant toxicity toward healthy cells, and are considered to be potential anticancer agents. However, little is known about their effects on prostate cancer cells. We synthesized and evaluated the effects of caffeic acid, CAPE (2) and 18 synthetic derivatives on cell viability and androgen-dependent cell proliferation, subcellular localisation and expression of androgen receptor (AR) and secretion of prostate-specific antigen (PSA) in LNCaP human hormone-dependent prostate cancer cells. Several synthetic derivatives of CAPE were strong, concentration-dependent cytotoxic agents in LNCaP cells with IC50 values in the 6.8-26.6 muM range, potencies that were up to five-fold greater than that of CAPE (33.7 ¡À 4.0 muM). A number of caffeic acid derivatives were inhibitors of androgen-stimulated LNCaP cell proliferation with concomitant inhibition of DHT-stimulated PSA secretion. Compound 24 was the most cytotoxic and antiproliferative caffeic acid derivative (IC50 values of 6.8 ¡À 0.3 and 2.4 ¡À 0.8 muM, respectively) inhibiting DHT-stimulated cell proliferation and PSA secretion statistically significantly at concentrations as low as 0.3 muM. Exposure to DHT increased cytoplasmic and nuclear AR levels and co-treatment with increasing concentrations of compound 24 or CAPE (2), notably, further increased these levels. In conclusion, a number of synthetic derivatives of caffeic acid are potent inhibitors of androgen-dependent prostate cancer cell proliferation and viability, acting, at least in part, via an antiandrogenic mechanism that involves increased nuclear accumulation of (presumably inactive) AR.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extended knowledge of (2,3-Dihydrobenzo[b][1,4]dioxin-5-yl)methanol

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PYRIDINONE DICARBOXAMIDE FOR USE AS BROMODOMAIN INHIBITORS

The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem