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Irradiation of trans-1-benzoyl-2-trans-styrylcyclopropane (IIa) and trans-1-p-toluoyl-2-trans-styrylcyclopropane (IIb), leads to formation of cis disubstituted cyclopropanes (IIIa) and (IIIb) respectively.However, photolysis of trans-1-trans-cinnamoyl-2-phenylcyclopropane (IV) results in isomerzation of the alpha,beta-double bond to produce V.Photolysis of trans-1-trans-p-methoxycinnamoyl-2-p-methoxyphenylcyclopropane (VI), by contrast, produces only a cyclobutane dimer formulated as (VII).Irradiation of 7-phenyl-3-benzylidenespiro<2.5>octan-2-one (IXb), under identical conditions, leads to isomerisation around the C=C bond.The structural assignments are based, interalia, on 13C NMR and 1H NMR spectral data.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A general procedure for synthesis of 5-phenyl-1,3-dioxane-4,6-dione derivatives is described. The synthesis involves the cycloaddition of (alpha- chlorocarbonyl)phenylketene with carbonyl compounds to generate the corresponding substituted 2-oxetanone’s which is readily transformed to the final products in one step. The 1,3-dioxane-4,6-dione is a rigid cyclic structure, and can undergo easy hydrolysis.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Dibenzylideneacetonedibromide (1) gives three different products 2, 3 and 4, when its solution in chloroform is irradiated by electromagnetic radiation at different wavelengths. The structures of these products have been confirmed by spectral analysis or co-TLC and mixed m.p. with authentic samples.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The direct Michael addition of enol acetates to alpha,beta-unsaturated ketones was achieved using a combination of Lewis acid catalysts, InCl 3 and Me3SiCl, which furnished stable enol-form products that could be further transformed into functionalized 1,5-diketones by reactions with various electrophiles.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A one-pot, diastereoselective synthesis of diverse azabicyclo[2.2.2]octanes from readily available starting materials is reported. The key strategy relies on creation of 2-aminoprop-1-ene-1,1,3-tricarbonitrile through dimerization of malononitrile which undergoes nucleophilic attack on dibenzalacetone at three sites leading to bicyclo[2.2.2]octanes.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A palladium-catalyzed intermolecular vicinal diarylation of terminal 1,3-dienes using aryldiazonium tetrafluoroborates and arylboronic acids is reported. Using this technology, two different arenes are regioselectively introduced in a vicinal fashion across the terminal alkene of a variety of terminal 1,3-dienes at ambient temperature. Through the action of a chiral bicyclo[2.2.2]octadienyl ligand at -20 C, good enantioselectivity has also been achieved.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A systematic and comparative study has been made starting from a naturally-occurring chalcone nucleus to design effective antibacterial agents. The present investigation established 1,5-bis(2-hydroxyphenyl)pent-1,4-diene-3- one (1c) as a lead compound with potential against a panel of pathogenic bacterial strains. Staphylococcus (coagulase negative), Escherichia coli, Pseudomonas aeruginosa, Acenetobacter sp. and Klebsiella pneumoniae. Gentamycine and tetracycline were used as reference drugs. The mode of antibacterial action of Ic was also studied by scanning electron microscopy, which showed membrane disruption and cell lysis of the organisms during the exposure of the tested compound. In vitro toxicity tests demonstrated that all the bioactive compounds showed far less toxicity against human erythrocytes.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Fluorination followed by the Michael addition or Robinson annulation of 1,3-dicarbonyl compounds is introduced for the synthesis of acyclic and cyclic alpha-fluoro-beta-ketoesters and alpha-fluoro-1,3-diketones. The decarboxylation step can also be added to the reaction sequence. High efficiency is achieved by the microwave heating and atom economic one-pot synthesis.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A reverse hydrogenolysis process has been developed for two-site coupling of 2-hydroxy-1,4-naphthoquinones with olefins to produce naphtha[2,3-b]furan-4,9-diones and hydrogen (H2). The reaction is catalyzed by commercially available Pd/C without oxidants and hydrogen acceptors, thereby providing an intrinsically waste-free approach for the synthesis of functionalized and potentially biologically relevant naphtha[2,3-b]furan-4,9-diones.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Osteosarcoma is a primary bone malignancy with aggressive metastatic potential and poor prognosis rates. In our earlier work we have investigated the therapeutic potential of curcumin as an anti-invasive agent in osteosarcoma by its ability to regulate the Wnt/beta-catenin signaling pathway. However, the clinical use of curcumin is limited owing to its low potency and poor pharmacokinetic profile. In this study, an attempt was made to achieve more potent Wnt inhibitory activity in osteosarcoma cells by carrying out synthetic chemical modifications of curcumin. We synthesized a total of five series consisting of 43 curcumin analogs and screened in HEK293T cells for inhibition of beta-catenin transcriptional activity. Six promising analogs, which were 6.5- to 60-fold more potent than curcumin in inhibiting Wnt activity, were further assessed for their anti-invasive activity and Wnt inhibitory mechanisms. Western blot analysis showed disruption of beta-catenin protein nuclear translocation following treatment with analogs 2f, 3c and 4f. Using transwell assays, we also found that these compounds were more potent than 1a (curcumin) in impeding the invasion of osteosarcoma cells, possibly through suppressing MMP-9 activity. Structure-activity-relationship studies revealed that Wnt inhibitory effects could be enhanced by shortening and restraining the flexibility of the 7-carbon linker moiety connecting the terminal aromatic rings of curcumin and substituting both rings with appropriate substituents. Our results demonstrate that the synthesized curcumin analogs are more potent Wnt inhibitors in osteosarcoma cell lines as compared to parental curcumin and are good lead compounds for further development. Future in vivo tests with these compounds will define their therapeutic potentials as promising drug candidates for clinical treatment of osteosarcoma.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate