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Direct carboxylation of simple arenes under atmospheric pressure of CO2 is achieved through a rhodium-catalyzed C-H bond activation without the assistance of a directing group. Various arenes such as benzene, toluene, xylene, electron-rich or electron-deficient benzene derivatives, and heteroaromatics are directly carboxylated with high TONs. This journal is

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Interesting scientific research on C8H9NO2

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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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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Compound 8H is a phenylcinnamide that induces G2/M-phase cell cycle arrest and cell death in cancer cell lines. Here we show that 8H exerts its cytotoxic activity through disruption of microtubule dynamics in vitro and in cell culture. A series of cinnamide derivatives were synthesized and evaluated, and several new compounds were identified that improve on the activity of the parent compound, with IC50 values for induction of cell death ranging from 1 to 10 muM. Notably, these compounds retain potency in the HL-60/VCR leukemia cell line, which is resistant to antimitotic cancer drugs vincrisitine and paclitaxel through up-regulation of P-glycoprotein drug efflux pumps. As P-glycoprotein expression is often responsible for drug resistance in cancer and the exclusion of compounds from the central nervous system, 8H and its derivatives merit further examination as potential antimitotic therapeutics, specifically for brain cancers and cancers that are resistant to standard antimitotic agents.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discover the magic of the C9H9BrO2

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The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R. sup.3 is hydroxy when the dashed line does not represent a covalent bond and R 3 is absent when the dashed line represents a covalent bond; R. sup.4 is (a), when X is O, a group of formula (i), (b), when X is O, NH or S, optionally substituted hydroxyphenyl, (c) an optionally substituted 4-to 7-membered heterocyclic ring, or (d), when X is NH, a group of formula (ii). The compounds are useful for the treatment of disease associated with the altered tone or motility of smooth muscle. STR1

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The Shocking Revelation of C8H9NO2

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Two series of nitrogenous heterocycle compounds-1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles have been synthesized and evaluated for their ALK5 inhibitory activity and cytotoxicity in TGFbeta-Smad2 assay and MTT assay, respectively. The ALK4/5/7 inhibitory activity of some compound was also evaluated in ALK4/5/7 autophosphorylation assays. Compounds 6c and 14c showed relatively potent ALK5 inhibition while weak cytotoxicity. At the same time, compounds 6c and 14c display relatively better ALK5 selectivity versus ALK4/ALK7 (nearly 10-fold) compared with SB431542, a well known ALK5 inhibitor. Compound 6g2 proved to be a moderately selective ALK4 inhibitor versus ALK5 and ALK7 (>10-fold). The binding mode of 14c generated by flexible docking study shows that 14c fits well into the site cavity of ALK5 by forming several tight interactions.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Properties and Exciting Facts About C9H9BrO2

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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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Benzodioxan,
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Final Thoughts on Chemistry for C9H9BrO2

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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 ± 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 ± 0.3 and 2.4 ± 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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Benzodioxan,
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Interesting scientific research on 22013-33-8

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The reaction of 3-formylchromones with aminoheterocycles was investigated. A simple and flexible general procedure for annulation of 5-(2-hydroxybenzoyl) pyridines was proposed. The best reaction conditions were found to be heating the reaction mixture in DMF in the presence of Me3SiCl as a promoter and water as scavenger. Georg Thieme Verlag Stuttgart.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extended knowledge of C10H10O3

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Employing simple and readily available aromatic ketones and anilines as starting materials resulted in the construction of 2-acylbenzothiazoles via a novel self-sequence reaction network, which assembles six reactions in one pot. The reaction network not only supplied a novel method for constructing complex molecules but also provided a typical example for logical self-organization synthesis.

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Benzodioxan,
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When the N,N-dialkylacetamide side chain of the highly ET(A)-selective endothelin antagonist ABT-627 (1; [2R,3R,4S]-2-(4-methoxyphenyl)-4-(1,3- benzodioxol-5-yl)-1-[[(N,N-dibutylamino)carbonyl]methyl]pyrrolidine-3- carboxylic acid; A-147627) is replaced by N,S-dialkylsulfonami-doethyl, the resultant analogs retain ET(A) affinity, but exhibit substantial ET(B) affinity as well. Structure-activity studies reveal that modifications in the length of the two alkyl groups, and in the substitution on the anisyl ring, are important in optimizing this ‘balanced’ antagonist profile. In particular the combination of an N-n-propyl group, an S-alkyl chain between four and six carbons in length, and a fluorine atom ortho to the aromatic OCH3 provides compounds with sub-nanomolar affinities for both receptor subtypes, and with ET(A)/ET(B) ratios close to 1. A number of these compounds also exhibit oral bioavailabilities (in rats) in the 30-50% range and have substantial plasma half-lives. The balanced receptor-binding profile of these potent and orally bioavailable compounds complements the ET(A) selectivity observed with 1.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem