• 제목/요약/키워드: structure-activity relationship

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문화역사적 활동이론을 통한 학부생 연구지원 프로그램 참여자의 과학연구 수행과정의 분석 (Analysis of the Scientific Research Process of a Participant in Undergraduate Research Program by Cultural Historical Activity Theory)

  • 이지원
    • 한국과학교육학회지
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    • 제38권3호
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    • pp.343-354
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    • 2018
  • 이 연구에서는 학부생 연구지원 프로그램(Undergraduate Research Program: 이하 URP)에 참여한 물리교육과 3학년인 한 초심자(학생 A)의 연구과정을 질적으로 분석하였다. 자료는 참여관찰, 심층인터뷰, 문서분석을 통해 수집되었고, 분석을 위한 이론적 틀로서 문화역사적 활동이론이 사용되었다. 먼저, 초심자의 연구를 위한 활동체계가 어떻게 구성되었는지를 살펴보았다. 연구 초기에 멘토가 대략적인 연구목표와 목표달성을 위한 매개체를 초심자에게 제공하였다. 연구주체인 학생 A는 동료 두 명을 모아, 자신이 이끄는 수직적 관계로 연구팀을 구성하였다. 이러한 역할분담은 과제특정지식, 연차, 그리고 참여율이 높을수록 의사결정권이 크다는 암묵적 규칙에 근거한 것이다. 다음으로, 활동체계의 변화 과정을 살펴보면, 크게 두 가지 모순이 변화의 원천이 되었다. 먼저 연구 초기에 멘토의 교육철학과 멘티의 교육적 요구 간의 모순이 발생하였다. 학생 A는 멘토의 인적 네트워크를 이용하여 외부의 활동체계에서 필요한 지식을 얻는 방식으로 모순에 의한 갈등을 극복하였다. 이렇게 획득한 지식을 이용하여 활동체계의 매개물(실험도구과 이론)을 정교화하였다. 두 번째 모순은 수평적 역할분담을 요구하는 팀 구성원들과 기존 역할분담을 고수하는 학생 A 간에 발생하였다. 학생 A가 팀 구성원들의 의견을 받아들인 후, 활동체계의 노동 분담 방식은 협력적으로 변화하였다. 마지막으로, 학생 A의 변화를 살펴보면, 학생 A는 연구 경험을 통해 교사의 길을 포기하고 과학자가 되기로 결심하였다. 또 학계 내의인적 네트워크를 생성하고 확장하게 되었으며, 협업에 대한 부정적인 마음가짐이 긍정적으로 바뀌게 되었다. 연구 초심자의 연구과정에 대한 활동체계의 구성과 변화의 분석을 통하여 사사교육의 지도 방식과 지원체계에 대한 시사점을 얻을 수 있다.

4-(Nitrobenzyl)Pyridine에 의한 알킬화합물들의 잠재적 변이원성에 대한 구조활성 및 광화학효과의 연구 (Photosensitization Effect and Structure-Activity Relationship on Mutagenic Potential of Alkylating Agents by 4-(Nitrobenzyl)Pyridine (4-NBP) test)

  • 김재현;엄애선;류재천
    • 한국환경성돌연변이발암원학회지
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    • 제21권1호
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    • pp.23-29
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    • 2001
  • The NBP assay was conducted to determine the photomutagenic or photocarcinogenic potential of alkylating agents. Using a 4-NBP in vitro technique, whereby photochemical treatment on CAS (Chemical Activation System) was performed to investigate the enhancement effect, 20 compounds were shown to undergo alkylating mechanisms with 4-NBP. Chemically meaningful results were obtained with different sets of 20 compounds for the alkylating activities due to the UV irradiation, demonstrating that all of the testing compounds showed increasing photoalkylating effects either in the presence or absence of CAS in comparison with previously reported data, except furoic acid and fumaric acid that showed decreasing effect in the presence of a CAS. Caffeine did not show a meaningful result either. However, these findings demonstrate the effects of potential photoalkylating activity in chemical activation system (CAS) and suggest a potential risk-ranking system for the in vivo assays.

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${\omega}$-피리딜 알켄산의 형태와 활성간의 상관관계 (The Correlation Between Conformations and Activities of ${\omega}$-Pyridylalkenoic Acids)

  • 이종달;도성탁
    • 약학회지
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    • 제41권3호
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    • pp.298-304
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    • 1997
  • Molecular mechanics and conformation search methods were carried oyt to investigate the relationship between conformations and thromboxane synthetase ingibitory activities of om ega-pyridylalkenoic acids. The initial geometries of ${\omega}$-pyridylalkenoic acids and heme part of cytochrome P-450 were obtained from MM+ geometry optimization. The bond lenths and angles were not varied by step during the conformation searching. Stable conformers of some ${\omega}$-pyridylalkenoic acids were obtained by comformational search method. The distances were 8.5~10.8 ${\AA}$- between N atom at 3-position of pyridine ring and C atom at carboxylic group of stable ${\omega}$-pyridylalkenoic acids. The conformations of ${\omega}$-pyridylalkenoic acids and heme part complex were determined by same method. In theses structures, benzene ring and ethylene group in ${\omega}$-pyridylalkenoic acids are making the structure more rigid and increase inhbitory activity. The electron donating groups in C atom shich is connected to pyridine ring also increase activity.

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Structure-activity Relationship Study of Fluoro-Neplanocin A as Potential Antiviral and Antitumor Agents

  • Shin, Dae-Hong;Moon, Hyung-Ryong;Choi, Won-Jun;Lee, Kang-Man;Lee, Sang-Kook;Jeong, Lak-Shin
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.245.3-246
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    • 2003
  • S-Adenosylhomocysteine hydrolase (SAH) catalyzes the hydrolysis of S-adenosylhomocysteine to adenosine and L-homocysteine and has been an attractive target for the development of broad spectrum antiviral agents. Based on the potent inhibitory activity of neplanocin A against SAH, we have reported the synthesis and novel mechanism of action of fluoro-neplanocin A. (omitted)

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A CoMFA Study of Quinazoline-based Anticancer Agents

  • Balupuri, Anand;Balasubramanian, Pavithra K.;Cho, Seung Joo
    • 통합자연과학논문집
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    • 제8권3호
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    • pp.214-220
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    • 2015
  • Cancer has emerged as one of the leading cause of deaths worldwide. A three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed on a series of quinazoline-based anticancer agents. Purpose of the study is to understand the structural basis for their inhibitory activity. Comparative molecular field analysis (CoMFA) technique was employed to develop 3D-QSAR model. Ligand-based alignment scheme was used to generate a reliable CoMFA model. The model produced statistically significant results with a cross-validated correlation coefficient ($q^2$) of 0.589 and a non-cross-validated correlation coefficient ($r^2$) of 0.928. Model was further validated by bootstrapping and progressive scrambling analysis. This study could assist in the design of novel and more potent anticancer agents.

Nob1e2-[3-(Cyclopentyloxy)-4-Methoxyphenyl]-1-Isoindolinone Derivatives. PartI: Synthesis and SAR Studies for the Inhibition of TNF-$\alpha$ Production

  • Park, Joon-Seok;Baik, Kyong-Up;Cho, Jae-Youl;Yoo, Eun-Sook;Byun, Young-Seok;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • 제24권5호
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    • pp.367-370
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    • 2001
  • This study describes the synthesis and in vitro evaluation of noble 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone Derivatives for the inhibition of TNF-$\alpa$ production. Among these compounds, 2- [3- (Cyclopentyloxy)- 4- methoxyphenyll- 3- methyl -1 - isoindolinone (5) was the most potent in inhibitory activity of TNF-$\alpa$ production in LPS-stimulated RAW264.7 cells.

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Naphthazarin Derivatives (Ⅶ): Antitumor Action against ICR Mice Bearing Ascitic S-180 Cells

  • Song, Gyu-Yong;Kim, Yong;You, Young-Jae;Gho, Hoon;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • 제24권1호
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    • pp.35-38
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    • 2001
  • Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydro-xyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1-Hydroxyiminoalkyl)-DMNQ derivatives expressed greater antitumor action than (1 -hydroxyalkyl)- or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher anti-tumor action than 2-sudstituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of > 400 %.

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Antitumor constituents from some Korean medicinal plants

  • Bae, Ki-Hwan
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.56-61
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    • 1998
  • For the screening of bioactive natural products, the benzene or methanol extracts from 93 medicinal plants of Korea were prepared, and tested for the cytotoxicity against L1210 cells and for the antitumor action (Bae et al., 1992 and 1996). Of 93 extracts tested, 6 samples showed a cytotoxicity in both benzene and methanol extract, 39 samples in benzene and 13 samples in methanol extract. The benzene extract of the root of Scutellaria indica L., Sophora fIavescens Solander ex Aiton, Carpesium abrotanoides L., Gymnaster koraiensis (Nakai) Kitamura, Pyrola japonica Klenze, and Forsythiae Fructus showed a potent cytotoxic activity. This observation led to isolate active cytotoxic components, some of which demonstrated some antitumor action. In addition, the structure-activity relationship was discussed.

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5-Arylidene-2(5H)-Furanone Derivatives: Synthesis and Structure-Activity Relationship for Cytotoxicity

  • Bang, Seong-Cheol;Kim, Yong;Yun, Mi-Young;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • 제27권5호
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    • pp.485-494
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    • 2004
  • Thirty-eight 5-arylidene-2(5H)-furanone derivatives possessing halo-, methoxy-, oxo-, dioxo-, and thiophenyl groups as well as anthraquinone and naphthquinone moieties were synthesized, and their cytotoxicity was evaluated against various cancer cell lines. The introduction of halogen atoms or nitro group at aromatic ring of 5-arylidene-2(5H)-furanone was shown to increase the cytotoxicity with 5-(3-nitrobenzylidene )-2(5H)-furanone (21) being the most potent. Among anthracenyl or naphthalenyl derivatives, (E)-5-[2-(1 ,4-dimethoxy-9, 10-dioxo) anthracenyl]-2(5H)-furanone (34) showed the most potent cytotoxic activity.