• Bulletin of the Korean Chemical Society
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• v.12 no.4
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• pp.371-373
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• 1991

The crystal structure of eprazinone dihydrochloride, $C_{24}H_{32}N_2O_2$${\cdot}$2HCl, has been determined from 2102 independent reflections collected on an automated Nonious CAD-4 diffractometer using graphite-monochromated $Mo-K\alpha$ radiation. The crystals are monoclinic, space group P$2_1$/n, with unit cell dimensions a=11.381(2), b=28.318(2), c=7.840(1) $\AA$, $\beta=92.45(2)^{\circ}$, ${\mu}=2.37$ c$m^{-1}$, F(000)=968, and Z=4. Final R value is 0.071 for independent 2102 observed reflections. The molecule assumes an extended conformation. The piperazine ring has a normal chair conformation and the four carbon atom are planar with a maximum displacement of 0.004 $\AA$ for C(18) atom. The two chloride ions are hydrogen bonded to the two piperazine nitrogen atoms [N(14)${\cdot}{\cdot}{\cdot}$Cl(1); 2.986(6) $\AA$ N(17)…Cl(2); 3.084(8) $\AA$].

• Bulletin of the Korean Chemical Society
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• v.35 no.8
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• pp.2438-2442
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• 2014

A kinetic study is reported for $S_NAr$ reaction of 1-fluoro-2,4-dinitrobenzene (5a) and 1-chloro-2,4-dinitrobenzene (5b) with alkali-metal ethoxides (EtOM, M = Li, Na, K and 18-crown-6-ether complexed K) in anhydrous ethanol. The second-order rate constant increases in the order $k_{EtOLi}$ < $k_{EtO^-}$ < $k_{EtONa}$ < $k_{EtOK}$ < $k_{EtOK/18C6}$ for the reaction of 5a and $k_{EtOLi}$ < $k_{EtONa}$ < $k_{EtO^-$ < $k_{EtOK}$ < $k_{EtOK/18C6}$ for that of 5b. This indicates that $M^+$ ion behaves as a catalyst or an inhibitor depending on the size of $M^+$ ion and the nature of the leaving group ($F^-$ vs. $Cl^-$). Substrate 5a is more reactive than 5b, although the $F^-$ in 5a is ca. $10pK_a$ units more basic than the $Cl^-$ in 5b, indicating that the reaction proceeds through a Meisenheimer complex in which expulsion of the leaving group occurs after the rate-determining step (RDS). $M^+$ ion would catalyze the reaction by increasing either the nucleofugality of the leaving group through a four-membered cyclic transition state or the electrophilicity of the reaction center through a ${\pi}$-complex. However, the enhanced nucleofugality would be ineffective for the current reaction, since expulsion of the leaving group occurs after the RDS. Thus, it has been concluded that $M^+$ ion catalyzes the reaction by increasing the electrophilicity of the reaction center through a ${\pi}$-complex between $M^+$ ion and the ${\pi}$-electrons in the benzene ring.

• Molecules and Cells
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• v.39 no.3
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• pp.217-228
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• 2016

To generate a biobetter that has improved therapeutic activity, we constructed scFv libraries via random mutagenesis of several residues of CDR-H3 and -L3 of hu4D5. The scFv clones were isolated from the phage display libraries by stringent panning, and their antiproliferative activity against HER2-positive cancer cells was evaluated as a primary selection criterion. Consequently, we selected AH06 as a biobetter antibody that had a 7.2-fold increase in anti-proliferative activity ($IC_{50}$: 0.81 nM) against the gastric cancer cell line NCI-N87 and a 7.4-fold increase in binding affinity ($K_D$: 60 pM) to HER2 compared to hu4D5. The binding energy calculation and molecular modeling suggest that the substitution of residues of CDR-H3 to W98, F100c, A101 and L102 could stabilize binding of the antibody to HER2 and there could be direct hydrophobic interactions between the aromatic ring of W98 and the aliphatic group of I613 within HER2 domain IV as well as the heavy and light chain hydrophobic interactions by residues F100c, A101 and L102 of CDR-H3. Therefore, we speculate that two such interactions were exerted by the residues W98 and F100c. A101 and L102 may have a synergistic effect on the increase in the binding affinity to HER2. AH06 specifically binds to domain IV of HER2, and it decreased the phosphorylation level of HER2 and AKT. Above all, it highly increased the overall level of p27 compared to hu4D5 in the gastric cancer cell line NCIN82, suggesting that AH06 could potentially be a more efficient therapeutic agent than hu4D5.

• Journal of Forest and Environmental Science
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• v.8 no.1
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• pp.21-33
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• 1992

This study was performed to investigate the hardness of wood related to the wood surface, sap and heartwood, early and latewood, specific gravity, annual ring width and moisture content on major Korean tree species such as Pinus koraiensis, Abies holophylla, Larix leptolepis and Quercus valiabilis. The results were summarized as follows: 1. The arithmetic mean values of wood hardness on cross section were respectively $8.0kg/mm^2$ on Quercus valiabilis, $7.4kg/mm^2$ on Larix leptolepis, $5.1kg/mm^2$ on Pinus koraiensis and $4.7kg/mm^2$ on Abies hollophylla. 2. Generally hardness of wood on cross section was greater than the others and the proportion of cross section hardness to radial was respectively 2.8 on Quercus valiabilis, 2.6 on Larix leptolepis, 3.8 on Pinus koraiensis, and 4.1 on Abies holophylla and that proportion was tend to be decrease as specific gravity increased. 3. It was recognized that the hardness of sap and heartwood was different from each of the tree species and generally heartwood hardness was somewhat greater than sapwood. 4. Generally latewood hardness with in a ring was greater than earlywood and the proportion of earlywood hardness to latewood decreased as specific gravity increased. 5. The relations between hardness of wood and specific gravity show a high positive correlation on all sample tree species. 6. The values of hardness decreased with increasing annual ring width. 7. Hardness of wood on Abies holophylla was greatest in oven dried wood and it was decreased as moisture content increased, but not changed with moisture content abve F.S.P.. The proportion of oven dried wood hardness to green are respectively 3.0 on cross, 2.4 on radial and 1.9 on tangential section.

• Journal of the Korean Institute of Electrical and Electronic Material Engineers
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• v.17 no.5
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• pp.508-514
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• 2004

A fluxgate magnetic sensor consists of a solenoid excitation coil, pick-up coil, and magnetic core. We presents the effect of magnetic core shape in a micromachined fluxgate sensor. To observe the performance of fluxgate sensor with magnetic core side width and gap, side width of 125 ${\mu}{\textrm}{m}$, 250 ${\mu}{\textrm}{m}$, and 500 ${\mu}{\textrm}{m}$ were designed in a rectangular-ring shaped core and the gaps of 0 ${\mu}{\textrm}{m}$, 50 ${\mu}{\textrm}{m}$, and 100 ${\mu}{\textrm}{m}$ were also fabricated in a racetrack shaped core. The solenoid coils and magnetic core were separated by benzocyclobutane(BCB) which had high insulation and good planarization characters. Copper coil patterns of 10 ${\mu}{\textrm}{m}$ width and 6${\mu}{\textrm}{m}$ thickness were electroplated on Ti(300 $\AA$) / Cu(1500 $\AA$) seed layers. 3 ${\mu}{\textrm}{m}$ thick N $i_{0.8}$F $e_{0.2.}$(permalloy) film for the magnetic core was also electroplated under 2000 gauss to induce the magnetic anisotropy. The magnetic core had the high DC effective permeability of ∼1,300 and coercive field of ∼0.1 Oe. Because the magnetic cores of 500 ${\mu}{\textrm}{m}$ side width and 0 gap had a low magnetic flux leakage, high sensitivity of ∼350 V/T were measured at excitation condition of 3 $V_{P-P}$ and 2 MHz square wave. The power consumption of ∼14 ㎽ was measured. The fabricated fluxgate sensor had the very small actual size of 3.0${\times}$1.7 $\textrm{mm}^2$. When two fluxgates were perpendicularly aligned in terrestrial field, their two-axis output signals were very useful to commercialize an electronic azimuth compass for the portable navigation system.m.m.m.

• Biomolecules & Therapeutics
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• v.32 no.2
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• pp.205-213
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• 2024

Hydroxychavicol, a primary active phenolic compound of betel leaves, previously inhibited bone loss in vivo by stimulating osteogenesis. However, the effect of hydroxychavicol on bone remodeling induced by osteoclasts is unknown. In this study, the anti-osteoclastogenic effects of hydroxychavicol and its mechanism were investigated in receptor activator of nuclear factor kappa-B ligand (RANKL)-induced osteoclasts. Hydroxychavicol reduced the number of tartrate resistance acid phosphatase (TRAP)-positive multinucleated, F-actin ring formation and bone-resorbing activity of osteoclasts differentiated from RAW264.7 cells in a concentration-dependent manner. Furthermore, hydroxychavicol decreased the expression of osteoclast-specific genes, including cathepsin K, MMP-9, and dendritic cell-specific transmembrane protein (DC-STAMP). For mechanistic studies, hydroxychavicol suppressed RANKL-induced expression of major transcription factors, including the nuclear factor of activated T-cells 1 (NFATc1), c-Fos, and c-Jun. At the early stage of osteoclast differentiation, hydroxychavicol blocked the phosphorylation of NF-κB subunits (p65 and Iκβα). This blockade led to the decrease of nuclear translocation of p65 induced by RANKL. In addition, the anti-osteoclastogenic effect of hydroxychavicol was confirmed by the inhibition of TRAP-positive multinucleated differentiation from human peripheral mononuclear cells (PBMCs). In conclusion, hydroxychavicol inhibits osteoclastogenesis by abrogating RANKL-induced NFATc1 expression by suppressing the NF-κB signaling pathway in vitro.

• The Korean Journal of Nuclear Medicine Technology
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• v.17 no.2
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• pp.59-66
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• 2013

Purpose: Recently, there is an increase of the number of hospitals using auto dispenser to reduce occupational radiation exposure when drawing up of the $^{18}F-FDG$ dose (5.18 MBq/kg) in a syringe from the dramatic high activity of $^{18}F-FDG$ multidose vial. The aim of this study is to confirm that using auto dispenser actually reduces the radiation exposure for technologists. Also we analyzed the reproducibility of auto dispenser to find optimized dispensing method for the device. Materials and Methods: We conducted three experiments. Comparison of radiation exposure on chest and hands: The chest and hands exposure dose received by technologists during the injection were measured by electronic personal dosimeter (EPD) and ring TLD respectively. Reproducibility of dispensed volume: We draw up the normal saline into 5 and 2 mL syringe using auto dispenser by changing the volume from 1 to 15 mm for 5 times in the same setting of the volume. The weight of 5 normal saline dispensed from the device at same volume was measured using micro balance and calculated standard deviation and coefficient of variation. Reproducibility of dispensed radioactivity: We dispensed 362.6 $MBq{\pm}10%$ of $^{18}F-FDG$ in 5 and 2 mL syringes from the multidose vial of different specific activity. In the same setting of volume, we repeated dispensing for 4 times and compared standard deviation and coefficient of variation of radioactivity between 5 syringes. Results: There was significant difference in the average of chest exposure dose according to the dispensing methods (P<0.05). Also, when dispensing $^{18}F-FDG$ in manual method, exposure dose was 11.5 times higher in right hand and 4.8 times higher in left hand than in auto method. In the result of reproducibility of dispensed volume, standard deviation and coefficient of variation shows decline as the dispensing volume increases. As a result of reproducibility of dispensed radioactivity, standard deviation and coefficient of variation increases as the specific activity increases. Conclusion: We approved that the occupational radiation exposure dose of technologists were reduced when dispensing $^{18}F-FDG$ using auto dose dispenser. Secondly, using small syringes helps to increase reproducibility of auto dose dispense. And also, if you lower the specific activity of $^{18}F-FDG$ in multidose vial below 915-1,020 MBq/mL, you can use auto dispenser more effectively keeping the coefficient of variation lower than 10%.

• Journal of the Korean Chemical Society
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• v.38 no.4
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• pp.283-287
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• 1994

The crystal stucture of bithional surfoxide, $C_{12}H_6Cl_4O_3S$, has been determined from 2295 independent reflections collected on an automated CAD-4 diffractometer with a graphite-monochromated $Mo-K\alpha$ radiation. The crystal belongs to the monoclinic, space group P2$_1$/n, with a unit cell dimensions a = 12.448(4), b = 9.740(1), c = $11.815(2)\AA$, $\beta$ = $100.06^{\circ}$, $\mu$ = 9.02 cm$^{-1}$, Dm = 1.76 g/cm$^3$, Dc = 1.75 g/cm$^3$, F(000) = 744, and Z = 4. The structure was solved by the direct method and refined by the least-squares method. The final R values was 0.037 for 2295 independent reflections. Overall conformation of the molecule is folded with respect to central surfur atom. Comparing with the molecular conformation of bithional, one of phenyl rings was swinged with about $180^{\circ}.$ This conformational change in the molecule results in the existance of intramolecular-hydrogen bond of S-O(3)---H-O(1) type and its steric hindrance between this moiety and the other phenyl ring. The two best planes of the phenyl rings have a maximum deviation of 0.009 $\AA$ for C(1) atom. The dihedral angle between two phenyl rings is $99.22^{\circ}.$ In the crystal structure, the molecules are packed with intermolecular-hydrogen bond of O(3)---H-O(2).

• The Journal of Korean Institute of Electromagnetic Engineering and Science
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• v.29 no.11
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• pp.821-827
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• 2018

In devices used for re-forming osteoblasts to treat osteoporosis, a magnetic field is applied from the outside of the bone, and the minerals contained in the bone are aligned in a certain direction and undergo precessional motion. When a $90^{\circ}$ RF pulse is applied by using an RF coil, protons of minerals are brought to an excited state, and phosphorus activity promoting the deposition of osteoblasts in the bone is increased, thereby reshaping the bone. Miniaturizing the RF coil that generates a signal corresponding to the harmonic of the precessional motional frequency by means of the $90^{\circ}$ RF pulse can drastically reduce the overall size of the bone reshaping system. In this study, we propose a methodology for the miniaturization of the RF coil that can be used for osteoblast re-formation using a bone reshaping system. The capacitance of the designed RF coil is 25 pF, the inductance is approximately 100 nH, and the resonance frequency is 96 MHz. The radius of the end ring of the designed RF coil is 18 cm, and the total length of the leg is $2{\times}11.6cm$. The performance of the coil is verified through post-design measurement.

• The Korean Journal of Pesticide Science
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• v.4 no.2
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• pp.21-28
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• 2000

A new fourty six 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenylpro- pionamide derivatives were synthesized and the herbicidal activities against rice plant and barnyard grass with pre-emergence in down land were measured. The structure activity relationships (SAR) between the activities and physicochemical parameters of the substituted(X) N-phenyl group in substrates were analyzed and discussed by Free- Wilson and Hansch method from the basis on the former study (Sung. et. al., 1999). The conditions of selective herbicide activity both the barnyard grass and rice plant are shown that the optimal hydrophobicity, $({\pi})_{opt.}=1.34$ and electron donating with field effect (F<0) of meta and ortho, para-substituted mono or disubstituent on the N-phenyl ring were found to contribute significantly. The herbicidal activities against barnyard grass are roughly the same as the results in up land whereas damage to rice plant in down land more increase than that of up land. Degradation products in water are 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)propionic acid ((A)) (obs. pKa=4.35 & obs. logP=4.77) and 6-chloro-2-benzoxazolone (B) (obs. pKa=8.40 & obs. logP=2.90). These results were supposing that the hydrolysis product of substrates, (A) is comparatively absorbed in rice plant but not in barnyard grass. And it is assumed from the SAR equations that the 2,6-dimethyl-4-methoxymethyl group substituent ($pI_{50}=5.41$, 3g/ha) is selected as the most highest herbicidal activity against barnyard grass in green house.