• Title/Summary/Keyword: A549 cell

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Novel Benzoylurea Derivatives as Potential Antitumor Agents; Synthesis, Activities and Structure-Activity Relationships

  • Hwang, Ki-Jun;Park, Kyung-Ho;Lee, Chong-Ock;Kim, Beom-Tae
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.781-785
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    • 2002
  • A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

Cytotoxic Compounds from the Stem Bark of Magnolia obovata

  • Min, Byung-Sun;Youn, Ui-Joung;Bae, Ki-Hwan
    • Natural Product Sciences
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    • v.14 no.2
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    • pp.90-94
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    • 2008
  • Two sesquiterpenes (1 - 2), a tetralone (3), and two phenylpropanoids (4 - 5) were isolated from the stem bark of Magnolia obovata Thunberg (Magnoliaceae) through repeated column chromatography. Their structures were identified as ${\beta}-eudesmol$ (1), cryptomeridiol (2), 4R-4,8-dihydroxy-${\beta}-tetralone$ (3), trans-pcoumaryl aldehyde (4), and p-coumaric acid (5) on the basis of spectroscopic analysis including two dimensional NMR and mass. Compounds 1 - 3 were tested in vitro for their cytotoxic activity against the K562, HeLa, A549, and HCT116 cancer cell lines. However, compounds 1 - 3 were inactive in this assay system.

Synthesis and in vitro Cytotoxicity Monoterpenoid as New Antitumor Agents (Monoterpenoid계의 새로운 항암제 합성 및 In vitro 세포독성 평가)

  • 이민정;김대근;백형근;이강노;정규혁
    • Biomolecules & Therapeutics
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    • v.9 no.3
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    • pp.143-155
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    • 2001
  • Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.

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Compounds from the Aerial Part of Saururus chinensis and Their Cytotoxic Activity

  • Min, Byung Sun;Tran, Thi Thu Trang
    • Natural Product Sciences
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    • v.18 no.4
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    • pp.227-232
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    • 2012
  • Ten known compounds, 7-hydroxysauchinone (1), sauchinone (2), di-O-methyltetrahydrofuriguaiacin B (3), henricine (4), saucerneol K (5), meso-dihydroguaiaretic acid (6), (-)-guaiacin (7), (3R,4S)-4-(4-hydroxy-3-methoxyphenyl)-4-methoxy-3-methylbutan-2-one (8), (E)-7-(4-hydroxy-3-methoxyphenyl)-7-methylbut-8-en-9-one (9), and licarin A (10), were isolated from aerial part of Sarurus chinensis. The chemical structures of these compounds were determined on the basis of spectroscopic analyses including 2D NMR. Compounds 1 - 10 were evaluated for their cytotoxic activity against the HL-60, MCF-7, and A549 cancer cell lines in in vitro.

The deformation space of real projective structures on the $(^*n_1n_2n_3n_4)$-orbifold

  • Lee, Jungkeun
    • Bulletin of the Korean Mathematical Society
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    • v.34 no.4
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    • pp.549-560
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    • 1997
  • For positive integers $n_i \geq 2, i = 1, 2, 3, 4$, such that $\Sigma \frac{n_i}{1} < 2$, there exists a quadrilateral $P = P_1 P_2 P_3 P_4$ in the hyperbolic plane $H^2$ with the interior angle $\frac{n_i}{\pi}$ at $P_i$. Let $\Gamma \subset Isom(H^2)$ be the (discrete) group generated by reflections in each side of $P$. Then the quotient space $H^2/\gamma$ is a differentiable orbifold of type $(^* n_1 n_2 n_3 n_4)$. It will be shown that the deformation space of $Rp^2$-structures on this orbifold can be mapped continuously and bijectively onto the cell of dimension 4 - \left$\mid$ {i$\mid$n_i = 2} \right$\mid$$.

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Cytotoxicity and Quantitative Analysis of Nortriterpenoid glycoside from Scilla scilloides (무릇에서 분리한 nortriterpenoid glycoside의 암세포에 대한 세포독성 및 함량 분석)

  • Lee, Sang-Myung;Chun, Hyo-Kon;Lee, Choong-Hwan;Lee, Ho-Jae;Kang, Shin-Jyung;Maeng, Hack-Young;Kho, Yung-Hee
    • Korean Journal of Pharmacognosy
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    • v.32 no.3 s.126
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    • pp.189-192
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    • 2001
  • Scillascilloside E-3 (1) and E-1 (2) were isolated from the bulbs of Scilla scilloides. The cytotoxic activities of these compounds were tested against murine (B16/F-10, 3LL) and human cancer cell lines (MCF7, PC-3, HT29, LOX-IMVI, A549 and HT1080). These compounds exhibited a significant cytotoxic activities against all tested cancer cells. Futhermore, the contents of 1 and 2 in S. scilloides are 43.2 and 27.9 mg/kg, respectively.

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Triterpenes from Perilla frutescens var. acuta and Their Cytotoxic Activity

  • Woo, Kyeong Wan;Han, Ji Young;Choi, Sang Un;Kim, Ki Hyun;Lee, Kang Ro
    • Natural Product Sciences
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    • v.20 no.2
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    • pp.71-75
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    • 2014
  • Nine triterpenes were isolated from the petroleum ether and MeOH extract of Perilla frutescens var. acuta leaves. Their structures were determined to be arjunic acid (1), maslinic acid (2), oleanolic acid (3), euscaphic acid (4), tormentic acid (5), 3-O-trans-p-coumaroyltormentic acid (6), 28-formyloxy-$3{\beta}$-hydroxy-urs-12-ene (7), ursolic acid (8), and corosolic acid (9) by spectroscopic methods. The compounds 1, 2, 4, 6, and 7 were isolated for the first time from this plant and the Genus Labiatae. The isolated compounds (1-9) were tested for cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro using a Sulforhodamin B bioassay.

Isoetin 5'-Methyl Ether, A Cytotoxic Flavone from Trichosanthes kirilowii

  • Rahman, Md. Aziz Abdur;Moon, Surk-Sik
    • Bulletin of the Korean Chemical Society
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    • v.28 no.8
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    • pp.1261-1264
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    • 2007
  • Bioassay-directed fractionations of the seed extracts of Trichosanthes kirilowii, have resulted in the isolation of two new compounds, 2-(4-hydroxy-3-methoxyphenyl)-3-(2-hydroxy-5-methoxyphenyl)-3-oxo-1-propanol (2) and isoetin 5'-methyl ether (5,7,2',4'-tetrahydroxy-5'-methoxyflavone) (3), together with two known compounds, 7-hydroxychromone (1) and 5,7,4'-trihydroxy-3',5'-dimethoxyflavone (tricin, 4). Their structures were characterized by spectroscopic analysis such as 2D-NMR, HRTOFMS, and UV. Compound 3 showed cytotoxicity against human lung cancer cell line A549, human skin melanoma SK-Mel-2, and mouse melanoma B16F1, with IC50 of 0.92, 8.0, and 7.23 μg/mL, respectively.

Guaiane Sesquiterpenoids from Torilis japonica and Their Cytotoxic Effects on Human Cancer Cell Lines

  • Park Hye Won;Choi Sang-Un;Baek Nam-In;Kim Sung-Hoon;Eun Jae Soon;Yang Jae Heon;Kim Dae Keun
    • Archives of Pharmacal Research
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    • v.29 no.2
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    • pp.131-134
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    • 2006
  • A new compound 2 and two known guaiane-type sesquiterpenoids were isolated from the methylene chloride-soluble fraction of the methanolic extract of the fruits of Torilis japonica (Umbelliferae) through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as torilin (1), 11-acetoxy-8-angeloyloxy-$1{\beta}$-hydroxy-4-guaien-3-one ($1{\beta}$-hydroxytorilin, 2), and 11-acetoxy-8-angeloyloxy-$1{\alpha}$-hydroxy-4-guaien-3-one ($1{\alpha}$-hydroxytorilin, 3) by spectroscopic analysis. Compounds 1-3 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.

Sterol Peroxide Derivatives from the Marine Sponge Spirastrella abata (국내산 해면 Spirastrella abata로부터 Sterol Peroxide 유도체의 분리)

  • Im, Kwang-Sik;Nam, Kyung-In;Sim, Chung-J.;Jung, Jee-H.
    • Korean Journal of Pharmacognosy
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    • v.31 no.4
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    • pp.401-406
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    • 2000
  • Marine sponges are known to be a source of diverse sterols. In our study on the cytotoxic components of the marine sponge Spirastrella abata, $5{\alpha},8{\alpha}-epidioxy\;{\Delta}^6$ sterols (1-5) and $5{\alpha},8{\alpha}-epidioxy\;{\Delta}^{6,9(11)}$ sterols (6-7) were isolated. The structures were identified based on the analyses of $^1H-NMR,\;^{13)C-NMR$, and MS data. These compounds were assayed for cytotoxicity against 5 human solid tumor cell lines including A549, SK-OV- 3, SK-MEL-2, XF498, and HCT15.

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