• Title/Summary/Keyword: $\mu$ synthesis

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Synthesis and Antitumor Evaluation of 3-(2-Chloroethyl)-hydantoins from Some Amino Acids (아미노산으로부터 3-(2-Chloroethyl) hydantoin들의 합성과 그들의 항암작용 평가)

  • 김정균;윤이규;고영심;윤웅찬;박무영;문경호
    • YAKHAK HOEJI
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    • v.27 no.4
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    • pp.309-314
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    • 1983
  • Six hydantoin derivatives, 3-(2-chloroethyl) hydantoin (6a), 3-(2-chloroethyl)-5-isopropylhydantoin (6b), 3-(2-chloroethyl)-5-isobutylhydantoin (6c), 3-(2-chloroetbyl)5-(2-butyl) hydantoin (6d), 3-(2-chloroethyl)-5-benzylhydantoin (6e), 3-(2-chloroethyl)-5-(indolyl-3-methyl) hydantoin (6f), were prepared by the treatment of the corresponding salt of amino acids with 2-chloroethyl isocyanate in cold water, followed by refluxing in concentrated HCl solution. Anticancer activity of the synthesized hydantoin derivatives were examined on murine leukemia L1210 cells growing in Fischer medium. Among them, 3-(2-chloroethy)-5-isobutyl-hydantoin (6c) showed substantially low $ED_{50}$ value of $9.6{\mu}g/ml$.

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Synthesis and Biological Activity of 6-Substituted-2-Oxo-Purine Nucleosides

  • Lee, Sang-Jun;Kim, Jong-Bae;Cho, Young-Ho;Kim, Jung-Han
    • Archives of Pharmacal Research
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    • v.17 no.3
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    • pp.170-174
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    • 1994
  • We have synthesized various 6-substituted 2-oxo-purine nucleosides from key intemediate, 6-[(4-methylphenylthio)-2-oxo-9(2, 3, 5tri-o-acetyl-$\beta$-D-ribofuanoslyl)]-2, 3- dihydropurine in relatively high yields by one step nucleophilic substitution. Various isoguanosine, xanthosine analogs and other 2-oxo-purine nucleosides containing nitrogen, sulfur and oxygen at C-6 of purine base were easily obtained by this method. The structures of the products were established on the basis of their spectral data studies. And cytotoxicity of resulting synthetic 6-substituted-2-oxo-purine nucleosides against some tumor cell-lines was examined. $Ed_{50}$ values of these synthetic compounds were above $100\;{\mu}g/ml$ except isoguanosine, $N^6$-methyl isoguanosine and thioxanthosine analogs.

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Synthesis and Biological Evaluation of New Allylamine Antimycotics (새로운 알릴아민 항진균제의 합성과 생물학적 평가)

  • Jeong, Byeong-Ho;Park, Eun-Ju;Mun, Hyeon-Ju;Yu, Jin-Cheol
    • YAKHAK HOEJI
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    • v.40 no.5
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    • pp.507-512
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    • 1996
  • Some allylamine compounds which are benzothiazole substituants in stead of naphthyl ring in naftifine, antifungal agents, were synthesized as potential antimycotics. The interme diate Schiff bases that were obtained by condensation of 2-aminobenzothiazole and trans-cinnamaldehyde, were reduced to imine compounds to give allylamines (5a-5d) after methylation. These compounds which were tested in vitro against five fungal cell lines containing Trichophyton mentagrophytes, showed no activity in 0.1~100${\mu}$g/ml range.

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Design of an efficient multiplierless FIR filter chip with variable length taps (곱셈기가 없는 효율적인 가변탭 FIR 필터 칩 설계)

  • 윤성현;선우명훈
    • Journal of the Korean Institute of Telematics and Electronics C
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    • v.34C no.6
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    • pp.22-27
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    • 1997
  • This paper propose a novel VLSI architecture for a multiplierless FIR filter chip providing variable-length taps. To change the number of taps, we propose two special features called a data-reuse structure and a recurrent-coefficient scheme. These features consist of several MUXs and registers and reduce the number of gates over 20% compared with existing chips using an address generation unit and a modulo unit. Since multipliers occupy large VLSI area, a multiplierless filter chip meeting real-time requirement can save large area. We propose a modified bit-serial multiplication algorithm to compute two partial products in parallel, and thus, the proposed filter is twice faster and has smaller hardware than previous multiplierless filters. We developed VHDL models and performed logic synthesis using the 0.8.mu.m SOG (sea-of-gate) cell library. The chip has only 9,507 gates, was fabricated, and is running at 77MHz.

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Synthesis and Conformation of Novel 4'-Fluorinated 5'-Deoxythreosyl Phosphonic Acid Nucleosides as Antiviral Agents

  • Kang, Lien;Kim, Eunae;Choi, Eun Joo;Yoo, Jin Cheol;Lee, Wonjae;Hong, Joon Hee
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4007-4014
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    • 2012
  • Efficient synthetic route to novel 4'-fluorinated 5'-deoxythreosyl phosphonic acid nucleosides was described from glyceraldehyde using Horner-Emmons reaction in the presence of triethyl ${\alpha}$-fluorophosphonoacetate. Glycosylation reaction of nucleosidic bases with glycosly donor 14 gave the nucleosides which were further phosphonated and hydrolyzed to reach desired nucleoside analogues. Synthesized nucleoside analogues 18, 21, 25 and 28 were tested for anti-HIV activity as well as cytotoxicity. Adenine derivatives 18 and 21 showed significant anti-HIV activity up to $100{\mu}M$.

Synthesis of Ergosterol and 5,6-Dihydroergosterol Glycosides and Their Inhibitory Activities on Lipopolysaccharide-Induced Nitric Oxide Production

  • Park, HoonGyu;Lee, Tae Hoon;Chang, Fei;Kwon, Hyun Ji;Kim, Jiyoung;Kim, Hakwon
    • Bulletin of the Korean Chemical Society
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    • v.34 no.5
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    • pp.1339-1344
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    • 2013
  • We have synthesized several glycosyl ergosterols and 5,6-dihydroergosterols (DHE) and examined their effects on production of nitric oxide (NO) and iNOS protein expression in LPS-treated RAW264.7 macrophage cells. Our results showed that DHE derivatives inhibited production of NO and iNOS protein expression more strongly than ergosterol derivative. Especially, DHE-Glc exhibited most potent inhibitory activity without cytotoxicity up to the concentration of $100{\mu}M$.

Synthesis and Preliminary Cytotoxicity Evaluation of New Diarylamides and Diarylureas Possessing 2,3-Dihydropyrrolo[3,2-b]quinoline Scaffold

  • Kim, Hyun-Jin;El-Gamal, Mohammed I.;Lee, Yong Sup;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2480-2486
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    • 2013
  • A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDA-MB-468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at $10{\mu}M$ concentration over those two cell lines were 84.97% and 87.13%, respectively.

Synthesis and Inhibition Effects on 5-HT6 Receptor of Benzothiazole Derivatives

  • Hayat, Faisal;Yoo, Euna;Rhim, Hyewhon;ParkChoo, Hea-Young
    • Bulletin of the Korean Chemical Society
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    • v.34 no.2
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    • pp.495-499
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    • 2013
  • A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-$HT_6$ ligands. In vitro assay was evaluated by measuring the 5-HT-induced $Ca^{2+}$ increases using HeLa cell line expressing the cloned human 5-$HT_6$ receptor, and the compound 13 showed potent 5-$HT_6$ receptor antagonistic effect with $IC_{50}$ value of 3.9 ${\mu}M$. Compound 13 also showed good selectivity on the 5-$HT_6$ over 5-$HT_4$ and 5-$HT_7$ receptors.

The Synthesis, NMR Sepectrum and MO Theoretical Studies on MBBA and EBBA (MBBA와 EBBA의 합성 NMR 스펙트럼과 분자궤도함수론적 연구)

  • Kim, Ui Rak;Jeon, Mu Sik;Kim, Un Seop;Chae, Yeong Bok
    • Journal of the Korean Chemical Society
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    • v.18 no.4
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    • pp.239-243
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    • 1974
  • By means of NMR spectrum analysis of the synthesized MBBA and EBBA, it has been found that benzene rings of p-n-butylaniline in both MBBA and EBBA molecules do not conjugate with the central double bond and the benzene ring is twisted from molecular plane of N-(p-methoxy or ethoxy benzylidene) group. And as a result of MO studies, the minimum energy conformation is found for the conformation of $30^{\circ}$ twisted angle. One sees reasonable agreement between theory and experiment.

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Facile Synthesis of Flower-like Superparamagnetic Fe3O4/BiOCl Nanocomposites as High Effective Magnetic Recyclable Photocatalyst under Visible Light

  • Wang, Wei;He, Mingyi;Zhang, Huan;Dai, Yatang
    • Journal of Magnetics
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    • v.21 no.2
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    • pp.179-182
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    • 2016
  • In this paper, 10 nm $Fe_3O_4$ nanoparticles were modified on the surface of $2{\mu}m$ flower-like bismuth oxychloride (BiOCl) spheres by a facile co-precipitation method. The results showed that the $Fe_3O_4/BiOCl$ nanocomposites exhibited excellent photocatalytic activity and superparamagnetic property ($M_s=3.22emu/g$) under visible light for Rhodamine B (RhB) degradation. Moreover, the $Fe_3O_4-BiOCl$ photocatalyst possessed magnetic recyclable property, which could maintain high photocatalytic effective even after 20 cycle times. These characteristic indicates a promising application for wastewater treatment.