• Title/Summary/Keyword: Indole Derivatives

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The 3D-QSAR Studies on the Indolinones Derivatives of PTKIs: CoMFA& CoMSIA

  • Kwack, In-Young;Kim, Chan-Kyung;Hyun, Kwan-Hoon;Lee, Bon-Su;Park, Hyung-Yeon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.186.3-186.3
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    • 2003
  • The three-dimensional quantitative structure-activity relationship (3D-QSAR) study using the comparative molecular field analysis (CoMFA) was performed on indolinones derivatives as an inhibitor of the protein tyrosine kinase of fibroblast growth factor receptor (FGFR). In the training set, twenty-four indolinone derivatives were aligned based on the indole fragment and the steric and electrostatic fields were included in the analysis. The best predicted model showed the cross-validated coefficient (r$^2$$\sub$cv/) of 0.804 and bib-cross validated coefficient (r$^2$) of 0.942. The CoMFA study can be used to predict several new inhibitors of the FGFR.

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Synthesis of Urea and Thiourea Derivatives and Their Inhibitory Activities of NO Production by Activated Macrophages (유레아 및 티오유레아 유도체의 합성과 활성화된 대식세포의 NO 생성 저해효과)

  • Kim, Yoon-Jung;Cheon, Ye-Jin;Lim, Hyo-Jin;Ryu, Jae-Ha;Jeon, Ra-Ok
    • YAKHAK HOEJI
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    • v.51 no.4
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    • pp.246-252
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    • 2007
  • Several ureas and thioureas were designed and synthesized and their inhibitory activities of NO production in lipopolysaccharide-activated macrophages were evaluated. Among these compounds, indole-containing thiourea 6e was the most potent showing 17.4 ${\mu}M$ of $IC_{50}$ value.

Improved growth and development in Suaeda glauca through exogenous treatment with indole-3-carboxylic acid

  • Kim, Ji-Young;Cho, Ei Ei;Lee, Seung Jae;Jeong, Jae-Hyeok;Chung, Nam-Jin
    • Proceedings of the Korean Society of Crop Science Conference
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    • 2017.06a
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    • pp.37-37
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    • 2017
  • Mechanistic studies of halophytes are urgent areas of agricultural research due to the increase in saline-contaminated and irrigated land worldwide. The halophyte Suaeda glauca (S. glauca) has advantages in terms of biomass and saline elimination due to its large mass and well-developed phenotype on seashores, although its mechanistic features and growing specificities still require systematic investigation. In this study, S. glauca was cultivated under various saline concentrations (0-400 mM) in Hoagland's solution in the absence or presence of indole derivatives to elucidate physiological features. The results confirmed the optimal growth and development of S. glauca in 50 mM NaCl, and morphologies such as the number of branches, shoot length, and fresh and dry weights were improved by indole-3-carboxylic acid (ICA) treatment. The cation concentrations in roots, shoots and leaves were investigated to examine the ionic imbalances in response to saline treatment, and the results demonstrated that sodium ions accumulated to high concentrations in leaves. The levels of calcium and potassium ions in roots were maintained or slightly decreased in the presence of 50 mM NaCl and proline concentration was increased significantly in roots at optimal concentrations. These results demonstrate that the concentrations of ions and metabolites are key regulators of optimal growth by regulating the physiology of halophytes.

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Dispersant-free Dyeing of Polyester with Temporarily Solubilized Azo Disperse Dyes from Indole Derivatives

  • Lee, Jung-Jin;Lee, Won-Jae;Kim, Jae-Pil
    • Fibers and Polymers
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    • v.4 no.2
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    • pp.66-70
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    • 2003
  • Temporarily solubilized azo disperse dyes based on 1,2-substituted indoles were synthesized and characterized. Dispersant-free dyeing of polyester by using the synthesized dyes has been investigated. The colour yields of the dyes on the polyester fabric were found to be highly dependent on the dyeing pH, optimum results being obtained at pH 5. The dyes exhibited good to excellent fastness properties on polyester while lightfastness was moderate.

A Study on syntheses of 3-(1'-Benzyl-2'-substituted indol-3'yl)-1-acrylophenone (3-(1'-Benzyl-2'-substituted indol-3'-yl)-1-acrylophenone유도체의 합성에 관한 연구)

  • Lee, Ki-Chang
    • Journal of the Korean Applied Science and Technology
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    • v.11 no.2
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    • pp.105-111
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    • 1994
  • Intermediates, 1-benzyl-2-substituted-3-carboxaldehyde[I]-[II], were prepared by the reaction of 2-substituted indole-3-carboxaldehyde with benzyl chloride. Indolylacrylophenone derivatives[III]-[X] were prepared from 1-benzyl-2-substituted-3-carboxaldehyde with acetophenone derivatives. They are as follows; 3-(1'-benzylindole-3'-yl)-1acrylophenone [III] 3-(1'-benzylindole-3-yl)-1(p-methoxy)acrylophenone [IV] 3-(1'-benzylindole-3-yl)-1(p-bromo)acrylophenone [V] 3-(1'-benzylindole-3-yl)-1(p-chloro)acrylophenone [VI] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-acrylophenone [VII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-methoxy)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-bromo)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-chloro)acrylophenone [X]

Chemical Constituents of Nelumbo nucifera Seeds

  • Rho, Taewoong;Yoon, Kee Dong
    • Natural Product Sciences
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    • v.23 no.4
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    • pp.253-257
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    • 2017
  • The phytochemical study for the extract of Nelumbo nucifera (Nymphaceae) seeds has led to the isolation of ten compounds including five simple phenolic compounds, two indole derivatives, a flavonoid glycoside, two abscisic acid derivatives. The interpretation of 1D and 2D NMR and ESI-Q-TOF-MS spectroscopic data revealed the chemical structures of isolates to be p-hydroxybenzoic acid (1), protocatechuic acid (2), (E)-p-coumaric acid (3), (E)-ferulic acid (4), (E)-sinapate-4-O-${\beta}$-$\text\tiny{D}$-glucopyranoside (5), tryptophan (6), 3-indoleacetic acid (7), isoschaftoside (8), dihydrophaseic acid (9), dihydrophaseic acid 3'-O-${\beta}$-$\text\tiny{D}$-glucopyranoside (10). To the best of our knowledge, 1 - 5 and 7 were identified for the first time from N. nucifera seeds, and the presence of dihydrophaseic acid (9) and its glucoside (10) were demonstrated secondly in this plant.

Indole Derivatives I, The Kinetics and Mechanism of the Nucleopilic Addition of Thiourea to 1-Benzylindole-3-Acetophenone (인돌유도체 I, 1-Benzylindole-3-acetophenone유도체에 대한 Thiourea의 친핵성 첨가반응 메카니즘과 그 반응속도론적 연구)

  • Lee, Ki-Chang;Hwang, Sung-Kwu;Ryu, Jung-Wook;Hwang, Young-Hyun;Sung, Ki-Chun
    • Journal of the Korean Applied Science and Technology
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    • v.8 no.2
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    • pp.175-181
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    • 1991
  • The kinetics of the addition of 1-benzylindole-3-(p-substituted) acetophenone derivatives was investigated by ultraviolet spectrophotometery in 30% dioxane -$H_2O\;at\;25^{\circ}C$. A rate equation which can be applied over wide pH range was obtained. The Substituent effects on 1-benzylindole-3-(p-substituted) acetophenone derivatives were studied, and addition were facilitated by electron attracting groups. On the base of the rate equation, substituent effect, and general base effect the plausible addition mechanism was proposed : Below pH 3.0, only neutral thiourea molecule was added to the carbon-carbon double bond, and in the range of pH 0.0${\sim}$14.0, netural thiourea molecule and thiourea anion competitively attacted the double bond. By contrast, above pH 10.0, the reaction was dependent upon only the addition of thiourea anion.

Research Trend about the Development of White Biotech-Based Aromatic Compounds (화이트바이오텍기반 방향족화합물 개발에 관한 연구동향)

  • Lee, Jin-Ho
    • Microbiology and Biotechnology Letters
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    • v.37 no.4
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    • pp.306-315
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    • 2009
  • Due to the depleting petroleum reserve, recurring energy crisis, and global warming, it is necessary to study the development of white biotech-based aromatic chemical feedstock from renewable biomass for replacing petroleum-based one. In particular, the production of aromatic intermediates and derivatives in biosynthetic pathway of aromatic amino acids from glucose might be replaced by the production of petrochemical-based aromatic chemical feedstock including benzene-derived aromatic compounds. In this review, I briefly described the production technology for hydroquinone, catechol, adipic acid, shikimic acid, gallic acid, pyrogallol, vanillin, p-hydroxycinnamic acid, p-hydroxystyrene, p-hydroxybenzoic acid, indigo, and indole 3-acetic acid using metabolic engineering, bioconversion, and chemical process. The problems and possible solutions regarding development of production technology for competitive white biotech-based aromatic compounds were also discussed.

Synthesis of Novel Hemicyanine Dyes for Color Compensating Film in Plasma Display Panels

  • Kim, Bo Hyung;Park, Se Woong;Lee, Donghyun;Kwon, Il Keun;Kim, Jae Pil
    • Bulletin of the Korean Chemical Society
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    • v.35 no.8
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    • pp.2453-2459
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    • 2014
  • Five novel cyanine dyes containing julolidine and indole moieties were synthesized. Several color compensating films for plasma display panels (PDP) were prepared using these dyes. The spectroscopic and physicochemical properties of the synthesized dyes in both solution and film state were evaluated. For each color compensating film, the optimum ratio of dye to binder was determined on the basis of transmittance, half band width, and photo-stability of the color compensating film. The five synthesized dyes showed sharp absorption peaks near 590 nm (orange light) and had molar extinction coefficients above $1{\times}10^5M^{-1}cm^{-1}$. The melting point of the dyes was above $200^{\circ}C$ and photo-stability of the color compensating films was improved by introducing substituents at the 5th position on the indole derivatives.