• Molecules and Cells
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• v.46 no.6
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• pp.387-398
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• 2023

Microtubule acetylation has been proposed as a marker of highly heterogeneous and aggressive triple-negative breast cancer (TNBC). The novel microtubule acetylation inhibitors GM-90257 and GM-90631 (GM compounds) cause TNBC cancer cell death but the underlying mechanisms are currently unknown. In this study, we demonstrated that GM compounds function as anti-TNBC agents through activation of the JNK/AP-1 pathway. RNA-seq and biochemical analyses of GM compound-treated cells revealed that c-Jun N-terminal kinase (JNK) and members of its downstream signaling pathway are potential targets for GM compounds. Mechanistically, JNK activation by GM compounds induced an increase in c-Jun phosphorylation and c-Fos protein levels, thereby activating the activator protein-1 (AP-1) transcription factor. Notably, direct suppression of JNK with a pharmacological inhibitor alleviated Bcl2 reduction and cell death caused by GM compounds. TNBC cell death and mitotic arrest were induced by GM compounds through AP-1 activation in vitro. These results were reproduced in vivo, validating the significance of microtubule acetylation/JNK/AP-1 axis activation in the anti-cancer activity of GM compounds. Moreover, GM compounds significantly attenuated tumor growth, metastasis, and cancer-related death in mice, demonstrating strong potential as therapeutic agents for TNBC.

• Journal of Pharmaceutical Investigation
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• v.17 no.2
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• pp.61-65
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• 1987

4-Pivaloyloxy, 4-benzenesulfonyloxy and 4-p-toluenesulfonyloxy compounds of piroxicam (2a, 2b and 2c) and isoxicam(4a, 4b and 4c) were synthesized in fairly good yield. Antiinflammatory and ulcerogenic effects of the 6 compounds were determined. Antiinflammatory effect of 2a was comparable to that of piroxicam and ulcerogenic effect of 2a was less than that of piroxicam.

• Archives of Pharmacal Research
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• v.17 no.5
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• pp.298-303
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• 1994

4-Arylazo-1H-pyrazol-3, 5-idimines 1a-c reacted with bromomalononitrile (2) to yield the corresponding imidazo[1, 2-b]pyrazoles 3a-c. The latter reacted with some active methylene compounds and with .alpha.-cinnamonitriles to afford the corresponding pyrazoloimidazopyridines 6, 8, 9 and 15, respectively. Compounds 3 reacted with each of formic acid, formamide, trichlo-roacetonitrile and with guanidine to yield the corresponding pyrazoloimidazopyrimidines 16-19 respectively.

• Food Science of Animal Resources
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• v.31 no.6
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• pp.879-885
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• 2011

This study was to identify and quantify the flavor compounds in cream cheese and cholesterol-removed cream cheese made from whole milk powder stored at $7^{\circ}C$ for 4 wk. Flavor compounds of cream cheese were identified using gas chromatography mass spectroscopy and quantified by gas chromatography. The tentatively identified flavor compounds were mainly eight from fatty acids in cream cheese made from whole milk powder (CCWMP) and nine from fatty acids in cholesterol-removed cream cheese made from whole milk powder (CRCCWMP). In quantitative analysis of the flavor compounds, most of the volatile compounds were slightly increased during storage. N-Decanoic acid was produced only in CCWMP. On the basis of the results, it was concluded that the quality and quantity of flavor compounds in CCWMP and CRCCWMP have almost no adverse effects in comparison with that of whole milk-made cream cheese.

• Archives of Pharmacal Research
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• v.29 no.10
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• pp.826-833
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• 2006

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

• Bulletin of the Korean Chemical Society
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• v.21 no.7
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• pp.679-684
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• 2000

The Sr2Co0.5Nb(Ta)0.5O4 and Sr3CoNb(Ta)O7 compounds, both with Ruddlesden-Popper structures, have been synthesized by the ceramic method at $1150^{\circ}C$ under atmospheric pressure. The crystallographic structure of the compounds was assigned to the tetr agonal system with space group 14/mmm by X-ray diffraction(XRD) Rietveld refinement. The reduced lattice volume and lattice parameters increased as the Ta with 5d substitutes for the Nb with 4d in the compounds. The Co/Nb(Ta)O bond length has been determined by X-ray absorption spectroscopic(EXAFS/XANES) analysis and the XRD refinement. The CoO6,octahedra were tetragonally distorted by elongation of Co-O bond along the c-axis. The magnetic measurement shows the compounds Sr2Co0.5Nb(Ta)0.5O4 and Sr3CoNb(Ta)O7 have paramagnetic properties and the Co ions with intermediate spin sates between high and low spins in D4h symmetry. All the compounds showed semiconducting behavior whose electrical conductivity increased with temperature up to 1000 K. The electrical conductiviy increased and the activation energy for the conduction decreased as the number of perovskite layers increased in the compounds with chemical formula An+1BnO3n+1.

• Nutrition Research and Practice
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• v.6 no.6
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• pp.491-498
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• 2012

Glycyrrhiza uralensis (or licorice) is a widely used Oriental herbal medicine from which the phenylflavonoids dehydroglyasperin C (DGC), dehydroglyasperin D (DGD), and isoangustone A (IsoA) are derived. The purpose of the present study was to evaluate the antioxidant properties of DGC, DGD, and IsoA. The three compounds showed strong ferric reducing activities and effectively scavenged DPPH, $ABTS^+$, and singlet oxygen radicals. Among the three compounds tested, DGC showed the highest free radical scavenging capacity in human hepatoma HepG2 cells as assessed by oxidant-sensitive fluorescent dyes dichlorofluorescein diacetate and dihydroethidium bromide. In addition, all three compounds effectively suppressed lipid peroxidation in rat tissues as well as $H_2O_2$-induced ROS production in hepatoma cells. This study demonstrates that among the three phenylflavonoids isolated from licorice, DGC possesses the most potent antioxidant activity, suggesting it has protective effects against chronic diseases caused by reactive oxygen species as well as potential as an antioxidant food additive.

• Bulletin of the Korean Chemical Society
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• v.27 no.6
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• pp.830-834
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• 2006

Lipid peroxidation induced by the reaction of cytochrome c with $H_2O_2$ was investigated. When linoleic acid micelles or phosphatidyl choline liposomes were incubated with cytochrome c and $H_2O_2$, lipid peroxidation was increased in cytochrome c and $H_2O_2$ concentrations-dependent manner. Radical scavengers, azide, formate and ethanol prevented lipid peroxidation induced by the cytochrome c/$H_2O_2$ system. Iron specific chelator, desferoxamine also prevented the cytochrome c/$H_2O_2$ system-mediated lipid peroxidation. These results suggest that lipid peroxidation may be induced by the cytochrome c/$H_2O_2$ system via the generation of free radicals. Carnosine, homocarnosine and anserine are present in the muscle and brain of many animals and human. Previous studies show that these compounds have an antioxidant function. In the present study, carnosine, homocarnosine and anserine significantly prevented the cytochrome c/$H_2O_2$ system-mediated lipid peroxidation. Carnosine and related compounds also inhibited the free radical-generating activity of cytochrome c. The results suggest that carnosine, homocarnosine and anserine may prevent lipid peroxidation induced by the cytochrome c/$H_2O_2$ system through a free radical scavenging.

• Korean Journal of Crystallography
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• v.8 no.1
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• pp.59-63
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• 1997

A method for the calculation of the idealized hydrogen positions in the following seven different kinds of compounds has been shown: (1) tertiary C-H, (2) secondary C-H, (3) $CH_3$ group with tetrahedral angles, (4) aromatic C-H or amide N-H, (5) O-H group with X-O-H angle tetrahedral, (6) terminal $X=CH_2$ or $X=NH_2^+$ with the hydrogen atoms in a plane and (7) acetylenic C-H with X-C-H linear.

• Journal of the Korean Chemical Society
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• v.40 no.5
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• pp.365-373
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• 1996

A series of new dimesogenic compounds, di-4-(p-substituted phenoxycarbonyl) phenoxyethyltetramethyldisiloxanes, were prepared and identified. Another compound having a $\beta$-naphthyl group in the place of a p-substituted phenyl ring was also synthesized. The results were as follows, 1) The compounds were synthesized with considerably high yields in the range of 85% to 95%. 2) All of the compounds are enantiotropic and form smectic phase in melt, the compound with $X=NO_2$ is $S_A$ while the remaining ones are SB. 3) Liguid crystalline phase transion of the compounds were influenced in corporations of the size and electron affinity of the substituent. 4) The heats of melting ΔHm, are particulary low, while the heats of isotropization, ΔHi, are comparable to other dimesogenic compounds. 5) The smectic group efficiency of the substituents in the compounds is in the order of $H