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Synthesis and Cytotoxicity of Some Rigid Derivatives of Methyl 2,5-Dihydroxycinnamate

  • Nam, Nguyen-Hai;Kim, Yong;You, Young-Jae;Hong, Dong-Ho;Kim, Hwan-Mook;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.590-599
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    • 2002
  • Eight rigid compounds designed as esterase-stable analogues of methyl 2,5-dihydroxycinnamate (1) were synthesized. These derivatives include 2-(2',5'-dihydroxybenzylidene)cyclopentenone (3a), 2-(2',5'-dihydroxybenzylidene)cyclohexanone (3b), 2,6-bis(2',5'-dihydroxybenzy-lidene)cyclohexanone (4b), 2,6-bis(2',5'-dihydroxybenzylidene)cyclopentenone (4a), (E)-3-(2',5'-dihydroxybenzylidene)pyrrolidin-2-one (5), (E)-5-(2',5'-dihydroxybenzylidene )-1,2-isothiazolidine-1,1-dioxide (6), 4-(2',5'-dihydroxyphenyl)-5H-furan-2-one (7), and 3-(2',5'-dihydroxyphenyl)cyclopent-2-ene-1-one (8). Among the eight compounds, the furanone 7 and cyclopentenone 8 showed the most potent cytotoxicity with $IC_{50}$ values of 0.39-0.98 $\mu\textrm{g}$/mL. Compound 8 was further brominated, phenylated and methylated at the a position to give three corresponding analogues, including 2-bromo-3-(2',5'-dihydroxyphenyl)cyclopent-2-ene-1-one (24), 3-(2',5'-dihydroxyphenyl)-2-phenylcyclopent-2-ene-1-one (27), and 3-(2',5'-dihydroxyphenyl)-2-methylcyclopent-2-ene-1-one (28). Among the three, the most enhanced activity was observed with the phenylated compound 27.

The Construction and Viterbi Decoding of New (2k, k, l) Convolutional Codes

  • Peng, Wanquan;Zhang, Chengchang
    • Journal of Information Processing Systems
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    • v.10 no.1
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    • pp.69-80
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    • 2014
  • The free distance of (n, k, l) convolutional codes has some connection with the memory length, which depends on not only l but also on k. To efficiently obtain a large memory length, we have constructed a new class of (2k, k, l) convolutional codes by (2k, k) block codes and (2, 1, l) convolutional codes, and its encoder and generation function are also given in this paper. With the help of some matrix modules, we designed a single structure Viterbi decoder with a parallel capability, obtained a unified and efficient decoding model for (2k, k, l) convolutional codes, and then give a description of the decoding process in detail. By observing the survivor path memory in a matrix viewer, and testing the role of the max module, we implemented a simulation with (2k, k, l) convolutional codes. The results show that many of them are better than conventional (2, 1, l) convolutional codes.

Effect of Prostaglandins $D_2,\;E_2\;and\;I_2\;on\;the\;Regulation\;of\;K_{ATP}$ Channel Activity in Rat Cardiac Myocytes

  • Ju, Jeong-Min;Nah, Seung-Yeol;Kim, Jae-Ha
    • The Korean Journal of Physiology and Pharmacology
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    • v.3 no.5
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    • pp.507-512
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    • 1999
  • Contribution of prostaglandins $D_2,\;E_2\;and\;I_2\;(PGD_2,\;PGE_2\;and\;PGI_2)$ on the regulation of ATP-sensitive $K^+$ channel $(K_{ATP}\;channel)$ was investigated in isolated single rat ventricular cardiac myocytes using the patch clamp technique. $PGD_2,\;PGE_2\;and\; PGI_2$ did not affect $K_{ATP}$ channel activity in the inside-out patch, but increased channel activity in a dose-dependent manner when the channel activities were attenuated by the administration of 100 ${\mu}M$ ATP to the internal solution in the inside-out patch. Channel activations by the prostaglandins were abolished by 50 ${\mu}M$ glibenclamide, a $K_{ATP}$ channel blocker. Dose-response curves of relative channel activity against the ATP concentrations of internal solution in the inside-out patch were shifted to the right in the presence of those three prostaglandins. The rank order of the channel stimulatory potencies $(as\;IC_{50}\;for\;ATP)$ calculated from the dose-response curves were $PGI_2\;>\;PGD_2\;>\;PGE_2.$ Conductance of the channel was not changed by those three prostaglandins. In conclusion, we suggest that prostaglandins $D_2,\;E_2\;and\;I_2$ are involved in the regulation of $K_{ATP}$ channel activity in certain circumstances, and that those three prostaglandins may cause myocardial relaxation by opening $K_{ATP}$ channels, thus protecting the heart from ischema.

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Aminolysis of 2,4-Dinitrophenyl and 3,4-Dinitrophenyl 2-Thiophenecarboxylates: Effect of ortho-Nitro Group on Reactivity and Mechanism

  • Seo, Jin-A;Chun, Sun-Mee;Um, Ik-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.29 no.8
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    • pp.1459-1463
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    • 2008
  • Second-order rate constants (kN) have been measured spectrophotometrically for reactions of 3,4-dinitrophenyl 2-thiophenecarboxylate (2) with a series of alicyclic secondary amines in 80 mol % $H_2O$/20 mol % dimethyl sulfoxide at 25.0 ${^{\circ}C}$. The Brønsted-type plot exhibits a downward curvature for the aminolysis of 2. The curved Brønsted-type plot is similar to that reported for the corresponding reactions of 2,4-dinitrophenyl 2- thiophenecarboxylate (1). The reactions of 1 and 2 have been suggested to proceed through the same mechanism, i.e., through a zwitterionic tetrahedral intermediate ($T^{\pm}$) with a change in the rate-determining step. Substrate 2 is less reactive than 1 toward weakly basic amines (e.g., $pK_a$ < 10.4) but becomes more reactive as the basicity of amines increases further. Dissection of kN into the microscopic rate constants has revealed that the reaction of 2 results in a smaller $k_2/k_{-1}$ ratio but larger $k_1$ than the corresponding reaction of 1. Steric hindrance exerted by the ortho-nitro group has been suggested to be responsible for the smaller $k_1$ value found for the reactions of 1.

Characterization of Dielectric Relaxation and Reliability of High-k MIM Capacitor Under Constant Voltage Stress

  • Kwak, Ho-Young;Kwon, Sung-Kyu;Kwon, Hyuk-Min;Sung, Seung-Yong;Lim, Su;Kim, Choul-Young;Lee, Ga-Won;Lee, Hi-Deok
    • JSTS:Journal of Semiconductor Technology and Science
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    • v.14 no.5
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    • pp.543-548
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    • 2014
  • In this paper, the dielectric relaxation and reliability of high capacitance density metal-insulator-metal (MIM) capacitors using $Al_2O_3-HfO_2-Al_2O_3$ and $SiO_2-HfO_2-SiO_2$ sandwiched structure under constant voltage stress (CVS) are characterized. These results indicate that although the multilayer MIM capacitor provides high capacitance density and low dissipation factor at room temperature, it induces greater dielectric relaxation level (in ppm). It is also shown that dielectric relaxation increases and leakage current decreases as functions of stress time under CVS, because of the charge trapping effect in the high-k dielectric.

Luminescence Wavelength Control of $CaAlSiN_3:Eu^{2+}$ by Ca-replacing: Computational and Experimental Study

  • Onuma, Hiroaki;Suehiro, Takayuki;Suzuki, Ai;Tsuboi, Hideyuki;Hatakeyama, Nozomu;Endou, Akira;Takaba, Hiromitsu;Kubo, Momoji;Sato, Tsugio;Miyamoto, Akira
    • 한국정보디스플레이학회:학술대회논문집
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    • 2009.10a
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    • pp.290-293
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    • 2009
  • We both theoretically and experimentally investigated the luminescence wavelength control of the $Eu^{2+}$-doped $CaAlSiN_3$ (CASN:$Eu^{2+}$). To modify emission wavelength, Na-doped and Mg-doped CASN:$Eu^{2+}$ (NCASN:$Eu^{2+}$ and MCASN:$Eu^{2+}$) have been studied. According to quantum chemistry calculation result, we synthesized NCASN:$Eu^{2+}$ and MCASN:$Eu^{2+}$. NCASN:$Eu^{2+}$ and MCASN:$Eu^{2+}$ showed shorter emission wavelength than that of CASN:$Eu^{2+}$.

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DNA Mediated Energy Transfer from 4',6-Diamidino-2-phenylindole to Ru(II)[(1,10-phenanthroline)2L]2+ : Effect of Ligand Structure

  • Youn, Mi-Ryung;Moon, Seok-Joon;Lee, Bae-Wook;Lee, Dong-Jin;Kim, Jong-Moon;Kim, Seog-K.;Lee, Chong-Soon
    • Bulletin of the Korean Chemical Society
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    • v.26 no.4
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    • pp.537-542
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    • 2005
  • It was proposed that Ru(II)[(1,10-phenanthroline)$_2$dipyrido[3,2-a:2',3'-c]phenazine ([Ru(phen)$_2$DPPZ]$^{2+}$)complexes and 4',6-diamidino-2-phenylindole (DAPI) simultaneously bind to poly[d(A-T)$_2$] (Biophysics. J. 2003, 85, 3865). Förster type resonance energy transfer from excited DAPI to [Ru(phen)2DPPZ]$^{2+}$ complexes was observed. In this study, we synthesized $\Delta$- and $\wedge$-[Ru(phenanthroline)$_2$dipyrido[3,2-a:2’3’c]6-azaphenazine] ([Ru(phen)$_2$DPAPZ]$^{2+}$) at which the DNA intercalating ligand DPPZ was replaced and we studied its binding properties to poly[d(A-T)$_2$] in the presence and absence of DAPI using polarized spectroscopy and fluorescence techniques. All the spectroscopic properties of the [Ru(phen)$_2$DPAPZ]$^{2+}$-poly[d(A-T)$_2$] complex were the same in the presence and absence of DAPI that blocks the minor groove of polynucleotide, suggesting both $\Delta$- and $\wedge$-[Ru(phen)$_2$DPAPZ]$^{2+}$ complexes are located at the major groove of poly[d(A-T)2]. On the other hand, in contrast with [Ru(phen)$_2$DPPZ]$^{2+}$, both $\Delta$- and $\wedge$-[Ru(phen)$_2$DPAPZ]$^{2+}$ exhibited almost twice the efficiency in the fluorescence quenching of DAPI that binds at the minor groove of poly[d(A-T)$_2$]. This observation indicates that the efficiency of the Förster type resonance energy transfer can be controlled by a small change in the chemical structure of the intercalated ligand.

The Measurement of Firing Noise of K2 Rifle at Close Distance (근접 측정에 의한 K2 소총 사격음의 측정)

  • 이윤
    • Transactions of the Korean Society for Noise and Vibration Engineering
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    • v.14 no.11
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    • pp.1123-1128
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    • 2004
  • An experimental study on firing noise of K2 rifle was performed. Firing noises of K2 rifle were measured at close distance to rifle. Firing noise of K2 rifle which made in Korea, has not measured before. The measurement of firing noise at close distance is not simple, because the amplitude of firing noise is much bigger than the measuring limit of ordinary sound level meter even though it uses a signal attenuator. The measurement of firing noise at close distance is necessary for noise source positioning and for obtaining the sound power of K2 rifle. By this experimental study, the firing noise levels of K2 rifle at different positions are obtained and these data can be used to Predict the sound pressure level at any distance from muzzle of the rifle. Also these data can be used to calculate the threshold shift of gunner's ear.

Studies on the Estimation of K2O Requirement for rice through the Chemical Test Data of Paddy Top Soil (화학분석(化學分析)을 통(通)한 수도(水稻)의 가리적량(加里適量) 추정(推定)에 관한 연구(硏究))

  • Kim, Moon Kyu
    • Korean Journal of Agricultural Science
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    • v.2 no.1
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    • pp.61-100
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    • 1975
  • This study has been made to find out the possibilty of successfully using the following $K_2O$ recommended equation $K_2O\;kg/10a=(Ko/\sqrt{Ca+Mg}-Ks/\sqrt{Ca+Mg})sqrt{Ca+Mg}.\;47.\;B\;D$. where $Ko/sqrt{Ca+Mg}=0.03518+0.0007658\;Sio_2/O.M$. $K_Ssqrt{Ca+Mg}$=Exchangeable K me/100g/$\sqrt{Total\;soluble(Ca+Mg)me/100g\;in\;Soil}$ B. D. =Bulk density of top soil, when the dose of Nitrogen for rice is estimated from the following equation: $N\;kg/10a=(4.2+0.096\;SiO_2/O.M).F$ where $F=0.907+0.263x-0.013x^2$ $SiO_2/O.M=(available\;SiO_2=ppm)/(organic\;matter\;%)$in soil For this. two field experiments. one in sandy and the other in clay paddy soil. have been conducted using 3 levels of wollastonite (0, 500, 100kg/10a) as main treatments; 3 levels of $K_2O$ application were used as sub-plots. These were as follows : (1) 8kg of $K_2O$/10a regardless of the K activity-$K/\sqrt{Ca+Mg}$; (2) kg of $K_2O$/10a estimated from the above equation. and (3) same as (2) above plus additional 30% of $K_2O$. The dose of N kg/ 10a was determined from the above equation based on the value of $SiO_2$/O.M. ratio in each treatment. There were three replications. The leading variety of rice in Chung Chong Nam Do area. Akibare (introduced from Japan) was used. The data obtained. through soil and plant analysis and growth and yield observations. have been throughly examined to attain the following summarized conclusions. 1. The nitrogen dose. estimated from the above equation. was in excess for optimum growth of the rice variety Akibare; indicating the necessity of modification onthe value of "F" or the constants in the equation. The concept of using $SiO_2$/O.M. in the equation was shown to be applicable. 2. The dose of potash. estimated from the respective equation given above. also was in excess of the rice requirements indicating the necessity of minor change in the estimation of $Ko/\sqrt{Ca+Mg}$ value and some great modification in the calculation of $Ks/\sqrt{Ca+Mg}$ value for the equation; however the concept of using $K/\sqrt{Ca+Mg}$ as a basis of $K_2O$ recommendation was shown to be quite reasonable. 3. It was found. from the correlation study using the data of paddy yield and amount of $K_2O$ absorbed by rice plants that the substitution of the value of $Ks/\sqrt{Ca+Mg}$ in the equation for the vaule $Ks/\sqrt{Ca+Mg}=0.037+0.78K\;me/100g$ soil was much more applicable than using the value calculated from the data of soil and wollastonite analysis.

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