- METHODS OF TREATMENT USING ARYLCYCLOPROPYLAMINE COMPOUNDS
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Described herein are methods of treating breast cancer using arylcyclopropylamine compounds.
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Paragraph 0303-0304
(2014/12/09)
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- Inhibitory effects of substituted cinnamic acid esters on mushroom tyrosinase
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A series of substituted cinnamic acid esters were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were evaluated. Compound 8 was found to be the most potent inhibitor with IC 50 value of 5.60μM. Preliminary structure activity relationships (SARs) were concluded. The inhibition kinetics analyzed by Lineweaver-Burk plots revealed that compound 8 was anti-competitive inhibitor.
- Zhang, Zhenghua,Liu, Jinbing,Wu, Fengyan,Zhao, Liangzhong
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p. 529 - 534
(2013/07/26)
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- METHODS OF TREATMENT USING ARYLCYCLOPROPYLAMINE COMPOUNDS
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Described herein are methods of treating Parkinson's disease using arylcyclopropylamine compounds.
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Paragraph 0221; 0222
(2013/07/19)
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- NOVEL FLAVANONE DERIVATIVE
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Provided is a novel antimicrobial agent. More specifically, provided is a novel antimicrobial agent capable of effectively acting on various resistant bacteria such as VSSA, MRSA, VISA, VRE, and VRSA. A novel flavanone derivative having a six-membered monosaccharide derivative, specifically, a glucose derivative or a galactose derivative is capable of effectively acting on the bacteria. More specifically, a compound represented by the general formula (I) is capable of effectively acting on the bacteria. (In the formula: X represents a six-membered monosaccharide derivative; and Y is substituted by a hydroxyl group.)
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Page/Page column 15
(2012/06/18)
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- Design, synthesis, and biological evaluation of new cinnamic derivatives as antituberculosis agents
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Tuberculosis, HIV coinfection with TB, emergence of multidrug-resistant TB, and extensively drug-resistant TB are the major causes of death from infectious diseases worldwide. Because no new drug has been introduced in the last several decades, new classes of molecules as anti-TB drugs are urgently needed. Herein, we report the synthesis and structure-activity relationships of a series of thioester, amide, hydrazide, and triazolophthalazine derivatives of 4-alkoxy cinnamic acid. Many compounds exhibited submicromolar minimum inhibitory concentrations against Mycobacterium tuberculosis strain (H37Rv). Interestingly, compound 13e, a 4-isopentenyloxycinnamyl triazolophthalazine derivative, was found to be 100-1800 times more active than isoniazid (INH) when tested for its ability to inhibit the growth of INH-resistant M. tuberculosis strains. The results also revealed that 13e does not interfere with mycolic acid biosynthesis, thereby pointing to a different mode of action and representing an attractive lead compound for the development of new anti-TB agents.
- De, Prithwiraj,Koumba Yoya, Georges,Constant, Patricia,Bedos-Belval, Florence,Duran, Hubert,Saffon, Nathalie,Daffé, Mamadou,Baltas, Michel
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p. 1449 - 1461
(2011/05/05)
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- Synthesis and anticancer activity evaluation of 2(4-alkoxyphenyl)cyclopropyl hydrazides and triazolo phthalazines
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A series of new 2(4-alkoxyphenyl)cyclopropyl hydrazide- and triazolo-derivatives were synthesized starting from 4-hydroxycinnamic acid (1) in a clean, mild, efficient and straightforward synthetic protocol. These compounds consisting of different alkoxy substitution, phenylcyclopropyl backbone and different heterocyclic groups were evaluated for in vitro anticancer activity against 4 cell lines displaying certain levels of resistance to pro-apoptotic stimuli and 2 cell lines sensitive to pro-apoptotic compounds. Compounds 7f and 8e were most active and displaying moderate in vitro cytostatic effect through different mechanisms. Significantly, chemically modified derivatives could be obtained in order to develop novel types of compounds aiming to combat apoptosis-resistant cancers, for example, those cancers associated with dismal prognoses.
- De, Prithwiraj,Baltas, Michel,Lamoral-Theys, Delphine,Bruyère, Céline,Kiss, Robert,Bedos-Belval, Florence,Saffon, Nathalie
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experimental part
p. 2537 - 2548
(2010/07/04)
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- ARYLCYCLOPROPYLAMINES AND METHODS OF USE
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Described herein are arylcyclopropylamine compounds that may inhibit enzymes comprising an amine oxidase domain, such as LSD1, MAO A and/or MAO B.
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Page/Page column 15-16
(2010/12/31)
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- Templating photodimerization of trans-cinnamic acid esters with a water-soluble Pd nanocage
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A water-soluble octahedral Pd nanocage acting as a reaction vessel templates the photodimerization of substituted trans-cinnamic acid methyl esters in water. Irradiation of the host-guest complexes of trans-cinnamic acid methyl esters with the Pd nanocage resulted in selective formation of a syn head-head dimer in addition to the corresponding cis isomer. These results suggest that the guest molecules are preoriented in a selective fashion with the hydrophilic ester group facing water and the hydrophobic aryl group tucked within the cavity of the host. Such an orientation occurs at the hydrophobic-hydrophilic interface between the nanocage exterior and interior. Weak intermolecular C-H-π and π-π interactions between the host and the guest(s) are likely to be responsible for the lack of mobility of the reactant olefins during their short excited-state lifetime.
- Karthikeyan,Ramamurthy
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p. 452 - 458
(2007/10/03)
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- Polarized Ketene Dithioacetals. 28. A New General Highly Stereoselective and Regiospecific Method for Homologation of Ketones to α,β-Unsaturated Esters via α-Oxoketene Dithioacetals
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A new highly stereoselective and regiospecific general method for the conversion of active methylene ketones to α,β-unsaturated O-methyl esters, S-methyl esters, and aldehydes via the corresponding oxoketene dithioacetals has been developed.Thus the carbinols 7a-g obtained by sodium borohydride reduction of the corresponding oxoketene dithioacetals 6a-g, derived from acetophenones and their higher homologues, have been shown to undergo boron trifluoride etherate assisted methanolysis to give the corresponding (E)-methylcinnamates 3a-d and their α-alkyl derivatives 3e-g in high yields.Also the acetals 6h-k derived from alkylmethyl ketones gave the corresponding (E)-methylcrotonates 3h-k.Similarly, the acetals 6l-p derived from alicyclic ketones gave the corresponding cyclic ene esters 3l-p under identical conditions.A few carbinols, 7a-d, were shown to undergo partial hydrolysis in the presence of boron trifluoride etherate/water to give the corresponding S-methyl thiocinnamates 8a-d.The cyclic acetals 6l-n were also similarly converted to the corresponding cyclic S-methylene thio esters 8e-g.The (methylthio)alkenyl ketones 20a-d and 18 after borohydride reduction and acidic hydrolysis gave the corresponding (E)-α,β-unsaturated aldehydes 22a-d and 19.The mechanism governing these transformations has been proposed.
- Myrboh, Bekington,Ila, Hiriyakkanavar,Junjappa, Hiriyakkanavar
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p. 5327 - 5332
(2007/10/02)
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