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Synthesis and Structure-activity Relationship of Cytotoxic $5,2^I,5^I$-Trihydroxy-7,8-dimethoxyflavanone Analogues

  • Min, Byung-Sun;Ahn, Byung-Zun;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.543-550
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    • 1996
  • Analogues of $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone, a naturally-occurring compound, which had been reported to have potent antitumor activity, were synthesized and examined for the cytotoxicity against three cancer cell lines. Among the intermediate chalcones and synthetic 5-hydroxy-7, 8-dimethoxyflavanone analogues, $({\pm})2^{l}, 5^{l}-dibenzyloxy-5, 7, 8-trimethoxyflavanone$ exhibited about 2-8 times stronger activity than $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone against L1210, K562 and A549 cancer cell lines. In the structure-activity relationship, it is suggested that among analogues of 5-hydroxy-7, 8-dimethoxyflavanone, the existence of two oxygenated groups of para-relation at $C-2^{I} and C-5^{I}$ positions on flavanone B-ring, may be necessary to exhibit effective cytotoxic activity.

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Synthesis and Biological Evaluation as a Potential Allylamine Type Antimycotics (알릴아민 항진균제의 합성과 생물학적 평가)

  • 정병호;조원제;천승훈;정순영;유진철
    • YAKHAK HOEJI
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    • v.47 no.5
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    • pp.293-299
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    • 2003
  • Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 4-fluorophenyl(2a-5a), 2-fluorophenyl(2b-5b), 2,4-dichlorophenyl(2c-5c), 2,6-dichlorophenyl(2d-5d), 4-nitrophenyl(2e-5e), and 2,3-dihydro-benzo[1,4]dioxan-6-yl( 2f-5f) instead of naphthyl group with hydrogen(3a-3f), methyl(4a-4f), and ethyl(5a-5f) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds(3a, 5a, 3c, 4c, 4d, 5d, 5e, and 4f) showed significant antifungal activity against T. mentagrophytes. (E)-N-Ethyl-(3-phenyl-2-propenyl)-4-nitro-benzenemethaneamine(5e) displayed moderate antifungal activity against all five different fungi.

Crystallization and Conductivity of $CuO-P_{2}O_{5}-Nb_{2}O_{5}-V_{2}O_{5}$ Glasses ($CuO-P_{2}O_{5}-Nb_{2}O_{5}-V_{2}O_{5}$ 유리의 결정화와 전기전도도)

  • 손명모;이헌수;구할본
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2000.11a
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    • pp.291-294
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    • 2000
  • The crystallization behavior and dc Conductivities of CuO-P$_2$O$_{5}$ -Nb$_2$O$_{5}$ -V$_2$O$_{5}$ glasses prepared by quenching on the copper plate were investigated. The conductivities of the glasses were range from 10$^{-5}$ s.$cm^{-1}$ / at room temperature, but the conductivities of the glass-ceramics were 10$^{-3}$ s.$cm^{-1}$ / increased by 10$^2$order. The crystalline product in the glass-ceramics was CuV$_2$O$_{6}$ . The linear relationship between in($\sigma$T) and T$^{-1}$ suggested that the electrical conduction in the present glass-ceramics would be due to a small polaron hopping mechanism.

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Effects of Dietary Supplementation of Ginkgo Leaf and Pumpkin on the Growth Performance, Intestinal Microflora, Blood Biochemical Profile and Antioxidant Status in Broiler Chickens (사료 내 은행잎과 호박 첨가 급여가 육계의 성장, 소장 내 미생물 균총, 혈액 생화학 분석 및 체조직 내 항산화 작용에 미치는 영향)

  • Ko, Young-Hyun;Lee, Seong-Sil;Jang, In-Surk
    • Korean Journal of Poultry Science
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    • v.37 no.1
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    • pp.23-33
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    • 2010
  • The current study was performed to develop natural bio-active substances as additives for the production of high quality broiler chickens. A total of 120 male 3 day-old broiler chicks were randomly allocated to CON (control), GK2.5 (ginkgo leaf 2.5%), GK5.0 (ginkgo leaf 5.0%), PK2.5 (pumpkin 2.5%) and PK5.0 (pumpkin 5.0%) of five groups in cages (24 birds per group). All birds were fed corresponding diets from 3 to 35 d of age and determined growth performance and biological parameters including blood biochemical profiles, antioxidant status and intestinal microflora. During the entire feeding trial, GK5.0 and PK5.0 groups resulted in a significantly (P<0.05) higher FCR than GK2.5 and PK2.5 groups. Plasma triglyceride significantly (P<0.05) increased in GK5.0 group compared with the other groups, and the level of alanine transaminase (ALT) increased (P<0.05) in GK5.0 and PK5.0 groups compared with that in PK2.5 group. Dietary addition of ginkgo leaf and pumpkin significantly (P<0.05) increased superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in the small intestine. Also, the addition of 2.5% ginkgo leaf significantly (P<0.05) increased the activities of SOD, GSH-Px and glutathione-S-transferase (GST) in the liver. Futhermore, muscle GST activity significantly (P<0.05) enhanced by dietary addition of ginko leaf and pumpkin. However, the level of lipid peroxidation (MDA) in the small intestine and muscle turned to be higher (P<0.05) in PK5.0 group. The colony forming units (CFU) of E. coli in intestinal digesta significantly (P<0.05) decreased in both ginko leaf and pumpkin supplemented groups compared with CON group. In conclusion, dietary addition of 2.5% ginko leaf and pumpkin as dietary sources can be applicable for the production of high quality broiler chickens.

Identification of Tumor Suppressor Loci on the Long Arm of Chromosome 5 in Primary Small Cell Lung Cancers (원발성 소세포폐암에서 염색체 5번의 장완에 위치한 종양억제유전자좌의 확인)

  • Cho, Eun-Song;Kim, Ho-Guen;Cho, Chul-Ho;Chang, Joon;Chung, Kyung-Young;Kim, Young-Sam;Park, Jae-Min;Kim, Sung-Kyu;Kim, Se-Kyu
    • Tuberculosis and Respiratory Diseases
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    • v.49 no.1
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    • pp.49-59
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    • 2000
  • Backgrounds : Recent cytogenetic studies indicated that long of the long arm of chromosome 5 is a frequent event in small cell lung canær (SCLC), suggesting the presence of a tumor suppressor gene in its place. To map the precise tumor-suppressor loci on the chromosome arm for further positional cloning efforts, we tested 15 primary SCLCs. Methods : The DNAs extracted from paraffin-embedded tissue blocks with primary tumor and corresponding control tissue were investigated. Nineteen polymorphic microsatellite markers located in the long arm of chromosome 5 were used in the microsatellite analysis. Results : We found that ten (66.7%) of 15 tumors exhibited LOH in at least one of tested microsatellite markers. Two (13%) of 10 tumors exhibiting LOH lost a larger area in chromosome 5q. LOH was observed in five common deleted regions at 5q. Among those areas, LOH between 5q34-qter and 5q35.2-35.3 was most frequent (75%). LOH was also observed in more than 50% of the tumors at four other regions, between 5q14-15 and 5q23-31, 5q31.1, 5q31.3-33.3, and 5q34-35. Three of 15 tumors exhibited shifted bands in at least one of the tested microsatellite markers. Shifted bands occurred in 2.5% (7 of 285) of the loci tested. Conclusion : Our data demonstrated that at least five tumor-suppressor loci exist in the long arm of chromosome 5 and that they may play an important role in small cell lung cancer tumorigenesis.

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A Study on the Band-pass Filters in Microstrip Parallel Coupled-Lines for W-LAN Applications (마이크로스트립 평행결합선 방식의 무선LAN용 대역통과필터에 관한 연구)

  • Park, Chang-Hyun;Kim, Young-Nam;Kim, Kab-Ki
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2008.05a
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    • pp.133-136
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    • 2008
  • In this paper, the parallel coupled line(PCL) band-pass filter satisfying IEEE 802.11a (a:$5.15{\sim}5.25$, b:$5.25{\sim}5.35$, c:$5.725{\sim}5.875$ [GHz]) has been designed for 5[GHz]band W-Lan RX-System applications. The designed PCL Band-Pass filter is of advantage to make a design formula that is small, light and approximate accuracy. It choose a microstrip plane figure because it is possible that a multiplicity of resonator was designed. It was shown that bandwidth was 14% from 5.15GHz to 5.92GHz at the -3dB designed filter. As a result, it is enough to use the designed filter at W-LAN RX-system of the 5GHz band.

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The Complexes of Aromatic Amines with Iodine or Iodine Monochloride in Carbon Tetrachloride (방향족아민과 요오드 또는 일염화요오드 사이의 錯物에 관한 연구)

  • Choi, Sang-Up;Lee, Bu-Yong
    • Journal of the Korean Chemical Society
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    • v.11 no.3
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    • pp.100-104
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    • 1967
  • The systems of aromatic amines such as aniline, N,N-dimethylaniline and N,N-diethylaniline with iodine or iodine monochloride in carbon tetrachloride have been examined spectrophotometrically. The results indicate the formation of one to one molecular complexes. The equilibrium constants obtained at room temperature for formation of the complexes are as follows: $C_6H_5NH_2{\cdot}I_2\;2.05$, $C_6H_5N(CH_3)_2{\cdot}I_2\;15.2$, $C_6H_5N(C_2H_5)_2{\cdot}I_2\;35.5$, $C_6H_5NH_2{\cdot}ICl\;18.5$, $C_6H_5N(CH_3)_2{\cdot}ICl\;25.6$, and $C_6H_5N(C_2H_5)_2\;42.0$ l $mole^{-1}$.

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Effects of $Nb_2O_5$ and $V_2O_5$ Additions on the Sintering Behavior and B-H Loop Properties of Lithium Ferrite ($Nb_2O_5$$V_2O_5$의 첨가가 Lithium Ferrite의 소결현상과 B-H Loop 특성에 미치는 영향)

  • 김현태;임호빈
    • Journal of the Korean Ceramic Society
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    • v.19 no.4
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    • pp.267-274
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    • 1982
  • The sintering behavior and B-H loop properties of $Li_{0.5O4}$ with the addition of $Nb_2O_5$ and $V_2O_5$ have been investigated by observation of microstructures and measurement of semi-static hysteresis loops. The sintering temperature was lowered by the additions of $Nb_2O_5$ and $V_2O_5$ and the effect of $V_2O_5$ addition was greater than that of $Nb_2O_5$. The abnormal grain growth was observed at about 100$0^{\circ}C$(d:4.6g/㎤) and 85$0^{\circ}C$(d:4.5g/㎤) in the specimens with the addition of $Nb_2O_5$ and $V_2O_5$ respectively. The addition of $Nb_2O_5$ retulted in a large and uniform grain size, and the addition of $V_2O_5$ resulted in a uniform grain size but the final density was lower than that of the pure specimen. The squareness was increased and the coercive force was decreased by the addition of $Nb_2O_5$, and the squareness was decreased and the coercive force was increased by the addition of $V_2O_5$. These effects could be explained by a large and uniform grain size, and by a lower final density of specimens with the addition of $Nb_2O_5$ and $V_2O_5$ respectively.

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A Comparison Study on the Separation Process of TaCl5 from the Chlorinated Reaction Product (염화반응법으로 제조된 TaCl5의 분리공정에 관한 비교 연구)

  • Cho, Jung-Ho;Park, So-Jin;Choi, Young-Yoon
    • Korean Chemical Engineering Research
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    • v.44 no.3
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    • pp.259-264
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    • 2006
  • The separation and purification of $TaCl_5$is indispensable in the synthetic process of $TaCl_5$by chlorination of tantalum oxide. The reaction products are mainly $TaCl_5$, $NbCl_5$, $TiCl_4$ and $FeCl_2$. However, we need to separate $TaCl_5/NbCl_5$ mixture from the reaction product, because $TaCl_5$ and $NbCl_5$ are easily separated each other by distillation or hydrogen reduction process. In this work, a comparison study was carried out between direct sequence and indirect sequence to obtain $TaCl_5/NbCl_5$ mixture from the reaction product by removing light component, $TiCl_4$ and heavy component, $FeCl_2$ using two distillation columns. It was concluded that the direct sequence gave better results than indirect sequence in the aspect of initial capital costs and the associative operating costs.

Electromigration Behavior of the Flip-Chip Bonded Sn-3.5Ag-0.5Cu Solder Bumps (플립칩 본딩된 Sn-3.5Ag-0.5Cu 솔더범프의 electromigration 거동)

  • Choi Jae-Hoon;Jun Sung-Woo;Won Hae-Jin;Jung Boo-Yang;Oh Tae-Sung
    • Journal of the Microelectronics and Packaging Society
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    • v.11 no.4 s.33
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    • pp.43-48
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    • 2004
  • Electromigration of Sn-3.5Ag-0.5Cu solder bumps was investigated with current densities of $3{\~}4{\times}10^4 A/cm^2$ at temperatures of $130{\~}160^{\circ}C$ using flip chip specimens which consisted of upper Si chip and lower Si substrate. Electromigration failure of the Sn-3.5Ag-0.5Cu solder bump occurred with complete consumption of Cu UBM and void formation at cathode side of the solder bump. The activation energies for electromigration of the Sn-3.5Ag-0.5Cu solder bump were measured as 0.61 eV at current density of $3{\times}10^4 A/cm^2$, 0.63 eV at $3.5{\times}10^4 A/cm^2$, and 0.77 eV at $4{\times}10^4 A/cm^2$, respectively.

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