• Title/Summary/Keyword: Rearrangement

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Synthesis and COX-2 Inhibitory Activity of Benzothiazine-3-carboxamide Derivatives (Benzothiazine-3-carboxamide 유도체의 합성과 COX-2 저해효과)

  • 신혜순;최희전;권순경
    • YAKHAK HOEJI
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    • v.46 no.6
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    • pp.375-380
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    • 2002
  • In this study, newly designed COX-2 inhibitors, synthetic derivatives of benzothiazine-3-carboxamide, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. 7-Bromo-1,2-benzoisothiazine derivatives were obtained from 4-bromotoluene over the chlorosulfonation, amination and oxidation. And benzothiazine ring was synthesized through Gabriel-Colmann rearrangement reaction. To evaluate inhibitory effect of COX-2, synthetic derivatives of benzothiazine-3-carboxamide were tested with accumulation of prostaglandin by lipopolysaccharide in aspirin-treated murine macropharge cell. Some of the synthesized lead compounds have potentially shown the structure-activity relationship for selectivity of COX-2 inhibition activity.

Searching biologically plausible synteny blocks among multiple genomes

  • Hachiya, Tsuyoshi;Sakakibara, Yasubumi
    • Proceedings of the Korean Society for Bioinformatics Conference
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    • 2005.09a
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    • pp.113-117
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    • 2005
  • In comparative genome analyses, synteny blocks play important roles for finding ortholog genes, reconstructing phylogenetic tree and predicting genome rearrangement events. In this paper, we propose a novel method to search biologically plausible synteny blocks not only from the viewpoint of finding highly preserved regions but also from the viewpoint of analyzing genome rearrangements. We have applied the method to our experiments on four fungal organisms, and succeeded to obtain some biologically interesting results.

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The basic study on the surface treatment of aluminum substract for lithography (평판인쇄용 Aluminum지지체의 표면처리에 관한 기초연구)

  • 황찬/
    • Journal of the Korean Graphic Arts Communication Society
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    • v.12 no.1
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    • pp.17-34
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    • 1994
  • Recently, the photopolymer made of novolak resin as the base and the naphthoquinonediazide(NQD) as the photoreactive compound is used for the presensitized plate(PS plate). The reaction mechanism of the NQD-novolak resin on light exposure is considered. Upon exposure it undergoes a Wolff rearrangement, via ketene intermediate which react with water ti form an 3-indene carboxylic acid. It was also found that NQD type resin in this experiment shows a high relative sensitivity compared with imported sample from Japan.

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Analysis for Scalar Mixing Characteristics using Linear Eddy Model (Linear Eddy Model을 이용한 스칼라의 혼합특성 해석)

  • Kim, Hoo-Joong;Kim, Yong-Mo;Ahn, Kook-Young
    • 한국연소학회:학술대회논문집
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    • 2004.06a
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    • pp.133-137
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    • 2004
  • The present study is focused on the small scale turbulent mixing processes in the scalar field. In order to deal with molecular mixing in turbulent flow, the linear eddy model is addressed. In each realization, the molecular mixing term is implemented deterministically, and turbulent stirring is represented by a sequence of instantaneous, statistically independent rearrangement event called by triplet map. The LEM approach is applied with relatively simple conditions. The characteristics of scalar mixing and PDF profiles are addressed in detail.

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Overview of ALK and ROS1 Rearranged Lung Cancer

  • Choi, Chang Min
    • Tuberculosis and Respiratory Diseases
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    • v.75 no.6
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    • pp.236-237
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    • 2013
  • Many attempts have been made to find genetic abnormalities inducing carcinogenesis after the development of epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor targeting EGFR in lung cancer. New target therapies have been already commercialized and studied along with the recent discovery of gene rearrangement involved in the carcinogenic process of non-small cell lung cancer. This study aims to investigate anplastic lymphoma kinase, c-ros oncogene 1, and receptor tyrosine kinase, in particular.

Synthesis of 6-[3-(Hydroxymethyl)-2, 3-epoxybutyl]-3, 5-dimethoxyphenol for the Preparation of Psorospermin (항암성 물질 Psorospermin의 합성중간체인 6-[3-(Hydroxymethly)-2, 3-epoxybutyl]-3, 5-dimethoxyphenol의 합성)

  • 고옥현
    • YAKHAK HOEJI
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    • v.30 no.6
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    • pp.329-333
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    • 1986
  • 6-[3-(Hydroxymethyl)-2, 3-epoxybutyl]-3, 5-dimethoxyphenol was synthesized by means of the eight steps, such as allylether, Claissen rearrangement, tosylation, oxidation, Wittig reaction, reduction and epoxidation from 3, 5-dimethoxyphenol. The epoxidation of 6-[3- (hydroxymethyl)-2-butenyl]-3,5-dimethoxy phenol using the L-(+)-diethyltartrate(DET), titanium (IV) isopropoxide Ti[(O-iPr)$_4$] and t-butylhydroperoxide(TBHP) is described.

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A Facile Synthesis of N,N'-Disubstituted Ureas from Amide and Amine by Using N-Bromophthalimide (NBP) and Silvercetate in One Pot

  • Park, Min-Soo;Choi, Chang-Uk
    • Archives of Pharmacal Research
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    • v.17 no.1
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    • pp.39-41
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    • 1994
  • Various N,N'-disubstituted ureas 5 were easily prepared from the corresponding primary amide 1 by tratment with N-Bromophthalimide $(NBP)-AgOAc-RNH$_{2}$ 4 in dry N,N-dimrthylformamide (DMF). This reaction envolved the intemediate formation of isocyanate 3 from amide 1 via Hofmann rearrangement by treatment with AgOAc and NBP and nucleophilic addition of amine 4 to this isocyante 3. This method is simple enough to be applied to the synthesis of various N,N'-disubstututed ureas scale conviently.

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PHOSPHATIDYLINOSITOL 3-KINASE REGULATES NUCLEAR TRANSLOCATION OF Nrf2 THROUGH ACTIN REARRANGEMENT

  • Kim, Sang-Geon;Kang, Keon-Wook;Lee, Seung-Jin;Park, Jeong-Weon;Kim, Hye-Jung
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.82-82
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    • 2002
  • Expression of phase II detoxifying genes is regulated by Nrf2-mediated antioxidant response element (ARE) activation. We previously showed that phosphatidylinositol 3-kinase (PI3-kinase) plays an essential role in ARE-mediated rGSTA2 induction by oxidative stress.(omitted)

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