• Title/Summary/Keyword: topoisomerase

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Synthesis, Cytotoxicity and Structure-Activity Relationship Study of Terpyridines

  • Zhao, Long-Xuan;Sherchan, Jyoti;Park, Jung-Ki;Jahng, Yurng-Dong;Jeong, Byeong-Seon;Jeong, Tae-Cheon;Lee, Chong-Soon;Lee, Eung-Seok
    • Archives of Pharmacal Research
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    • v.29 no.12
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    • pp.1091-1095
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    • 2006
  • For the development of novel antitumor agents, we designed and synthesized terpyridines, and their biological activities were evaluated. Although most of the newly prepared terpyridines showed strong cytotoxicity against several human cancer cell lines, [2,2';6',2"]-terpyridine displayed the most significant cytotoxicity.

A SURVEY OF N-STRING TANGLE ANALYSES OF DNA-ENZYME SYNAPTIC COMPLEXES

  • KIM, SOOJEONG;MOON, HYEYONG
    • Journal of applied mathematics & informatics
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    • v.35 no.3_4
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    • pp.349-369
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    • 2017
  • In last 30 years, mathematical tangle theory is applied to molecular biology, especially to DNA topology. The recent issues and research results of this topic are reviewed in this paper. We introduce a tangle which models an enzyme-DNA complex. The studies of 2-string tangle equations related to Topoisomerase II action and site-specific recombination is discussed. And 3-string tangle analysis of Mu-DNA complex, n-string tangle analysis ($n{\geq}4$) of DNA-enzyme synaptic complexes are also discussed.

Identification of Radiation-Sensitive Gene in U937 Cell by using cDNA-Chip Composed of Human Cancer Related Gene (U937 세포에서 발암관련 유전자들로 구성된 DNA chip을 이용한 방사선 감수성 유전자들의 선발)

  • 김종수;김인규;강경선;윤병수
    • Environmental Mutagens and Carcinogens
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    • v.22 no.1
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    • pp.54-59
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    • 2002
  • We have used cDNA microarray hybridization to identify gene regulated in response to gamma-irradiation in U-937 cell. The cDNA-chip was composed entirely of 1,000 human cancer related gene including apoptosis and angiogenesis etc. In gamma-irradiated U-937 cell, highly charged protein, ribosomal protein L32, four and a half LIM domains 3, lipocalin 2 (oncogene 24p3) and interleukin 15, ataxia telangiectasia mutated (includes complementation groups A, C and D) genes showed increased level of its transcription, and cell division cycle 25A, dihydrofolate reductase, topoisomerase (DNA) II beta(180kD), kinase suppressor of ras and strarigin genes showed reduced level of its transcription compared to untreated U-937 cell. The significant change of level of transcription was not found in well-known ionizing radiation(IR)-responsive gene, such as transcription factor TP53 and p53 related gene, except ataxia telangiectasia mutated gene.

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A New Stilbene Glucoside from the Roots of Polygonum multiflorum Thunb.

  • Xu, Ming-Lu;Zheng, Ming Shan;Lee, Yeon-Kyong;Moon, Dong-Cheol;Lee, Chong-Soon;Woo, Mi-Hee;Jeong, Byeong-Seon;Lee, Eung-Seok;Jahng, Yurng-Dong;Chang, Hyeun-Wook;Lee, Seung-Ho;Son, Jong-Keun
    • Archives of Pharmacal Research
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    • v.29 no.11
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    • pp.946-951
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    • 2006
  • One new stilbene glucoside (6), along with five known compounds (1-5), were isolated from the roots of Polygonum multiflorum Thumb., and their chemical structures established based on physicochemical and spectroscopic data. Of the compounds, compound 3 showed DNA topoisomerase I and II inhibitory activities.

A First Synthesis of Isofagar-idine:Topoisomerase I Inhibitor

  • Cho, Won-Jea;Miyoji Hanaoka
    • Archives of Pharmacal Research
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    • v.19 no.3
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    • pp.240-242
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    • 1996
  • We have reported the convenient biomimetic methodology for the synthesis of all kinds of substituent pattern benzo[c]phenanthridine alkaloids (Hanaoka et al., 1990; Hanaoka et al., 1991). Regioselective demethylation of C-8 position on oxyfagaridine (5), an intermediate for the synthesis of Fagaridine (4), would afford the precursor for the synthesis of Isofagaridine because the strong hydrogen bonding between amide and hydroxyl group of C-7 position probably resists to be reacted with week base and electrophiles. Thus, a selective alkylation of dihydroxy compound supposed to be possible and be lead to the target compound, Isofagaridine.

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Synthesis of Benzoquinoxalines

  • Kwon, Nam-Koong;Lee, Hee-Soon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.351.2-351.2
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    • 2002
  • We have previously reported the synthesis and cytotoxic activities of a series of azaanthraquinone derivatives on the model of doxorubicin(Dox). Dox is known to intercalate into DNA and to inhibit topoisomerase II activity. But in the case of Quinone compounds like Dox. its use is limited because of systemic toxicities. primarily cardiotoxicity and myelosuppression. In this study. we describe the synthesis of benzoquinoxaline derivatives as DACA analogue. DACA has a neutral chromophore and acridine moiety and posions both topoisomerases I and ll with DNA intercalating activity. In order to delineate the SAR of benzoquinoxaline derivatives. an effcient sythetic rout to the target compounds without quinone group. Various attempted removal of quinone from benzoquinoxlinedione was unsuccessful. Diels-Alder rout applied for the synthesis of the target compounds will be discussed.

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Isolation and Structure Determination of Cytotoxic Compounds with Topoisomerse I and II Inhibitory Activity from the spikes of Prunella vulgaris var. lilaeina

  • Byun, S.J.;Lee, J.E.;Son, J.K.;Lee, J.S.;Lee, S.H.;Park, Y.S.;Woo, M.H.
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.370.1-370.1
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    • 2002
  • Prunella vulgaris var. lilacina (Labiatae) has been used as a Korean traditional medicine for the treatment of. fever. inflammation. urinary disadvantage and cancer. We previously isolated three $\alpha$-amyrin triterpenoids from n-butanol-I extract. They are 3$\alpha$-hydroxyurs-12-ene-28-oic acid (ursolic acid). 2$\alpha$, 3$\alpha$-dihydroxyurs-12-ene-28-oic acid and 2$\alpha$. 3$\alpha$. 19$\alpha$ trihydroxyurs-12-ene-28-oic acid (euscaphic acid) exhibiting cytotoxicity and topoisomerase I inhibition. (omitted)

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Design and Synthesis of N-Aryl 8,9-Dihydro-7H-isoindolo[5,6-g]quinoxaline-7,9-dione Derivatives as Potential Antitumor Agent

  • Lee, Hee-Soon;Jung, Eun-Kyung;Nam, Koong-Kwon;Jung, Jae-Kyung
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.174.1-174.1
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    • 2003
  • We have previously reported the synthesis and cytotoxic activities of a series of azaanthraquinone derivatives using doxorubicin as a lead compound. Doxorubicin is known to intercalate into DNA and to inhibit topoisomerase II activity. But in the case of quinone compounds like Dox, its use is limited because of systemic toxicities, primarily cardiotoxicity and myelosuppression. In this study, we discuss the synthesis of isoindolobenzoquinoxaline derivatives. The quinone group of the azaanthraquinone derivatives were removed in the target compounds. (omitted)

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