• Title/Summary/Keyword: active agents

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Synthesis and In Vitro Cytotoxicity of 4-Alkyl- or 4-Arylaminosubstituted Cyclopenta[c]quinoline Derivatives

  • Lee, Hee-soon;Lee, Jee-man;Yang, Sung-Il
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.385-389
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    • 2001
  • Twelve 4-substituted cyclopenta[c]quinoline derivatives were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T-47D). The compounds 6c and 6e bearing p-anisidine and pyrrolidine side chain were more active than the others.

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Inhibitory Effect of Herbal Medicines on Rotavirus Infection (수종 생약의 로타바이러스 감염 억제효과)

  • Song, Mi-Jeong;Kim, Dong-Hyun
    • Korean Journal of Pharmacognosy
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    • v.29 no.2
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    • pp.125-128
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    • 1998
  • Sporadic diarrhea occurring predominantly in infants and young children is a significant illness of worldwide importance. Rotaviruses are the etiologic agents for 47% of the cases of infantile diarrhea in Seoul, Korea. This research was undertaken to investigate the inhibitory effect of traditional herbal medicines on rotatvirus infection. Among tested 50 kinds of herbal medicines, Coptidis Rhizoma was best on inhibitory activity of rotavirus infection, followed by Astragali Radix and Anthrisci Radix. The active component of Coptidis Rhizoma was berberine.

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Reactions with Heterocyclic Amidines $(Vl)^1$: Synthesis of some new sym. and assym. pyrazolotriazines and pyrazolo[4,5-e]pyrimidine derivatives

  • Ali Elagamey, Abdel Ghani
    • Archives of Pharmacal Research
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    • v.10 no.3
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    • pp.173-178
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    • 1987
  • Several new pyrazolo [1, 5-a]-S-triazine, pyrazolo [4, 5, -elpyrimidine, pyrazolo [1, 5-a] pyrimidine derivatives were synthesized via condensation of 3-antipyrinyl-5-amino-pyrazole (2) with $\beta$$-bifunctional reagents. The azo analogues of pyrazolo [1, 5-a] pyrimidines ; i. e. pyrazolo [5, 1, c]-as-triazine and pyrazolo[5, 1, -c]-as-benzotriazine were synthesized by coupling of diazotized 2-with agents containing active hydrogen.

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Efficient Synthesis of 2-Substituted 2,3-Dihydro-4-quinolones as Potential Intermediates for 2-Substituted 1,2,3,4-Tetrahydro-4-quinolone Antitumor Agents

  • Choi Sun;Jung Keumn-Yeo;Ryu Jae-Sang
    • Archives of Pharmacal Research
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    • v.29 no.5
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    • pp.369-374
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    • 2006
  • An efficient method for the synthesis of optically active 2-substituted 2,3-dihydro-4-quinolones has been developed. The key features include the introduction of a chiral side chain and the construction of quinolone skeleton by Mitsunobu alkylation and hydroarylation, respectively.

Synthesis and In Vitro Cytotoxicity of 1,3-Dioxoindan-2-Carboxylic Acid Arylamides

  • Jung, Jae-Kyung;Ryu, Jin-Hyeong;Yang, Sung-Il;Cho, Jung-Sook;Lee , Hee-Soon
    • Archives of Pharmacal Research
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    • v.27 no.10
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    • pp.997-1000
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    • 2004
  • A series of 1,3-dioxoindan-2-carboxylic acid arylamides were synthesized and evaluated for in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T- 47D). The most active was compound 3e (1.2 ${\mu}M$ against SK-OV-3 cell line) bearing a 4- methyl substituent.

Antilipid Peroxidative Effect of Houttuynia cordata (즙채의 과산화지질 생성 저해효과)

  • 김주향;양기숙
    • YAKHAK HOEJI
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    • v.45 no.5
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    • pp.494-499
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    • 2001
  • Houttuynia cordata (Saururaceae) has pungent smell and taste. It has been regarded as detoxicant, antipyretic, antiinflammantory and diuretic agents. In order to evaluate antioxidative and antilipidperoxidative efficacies, its fractions ($H_2O$, 20% MeOH, 40% MeOH, 60% MeOH, 170% MeOH) were measured by DPPH method and TBARS assay on rat liver homogenate. It was revealed that 60% MeOH fractions had potential antioxidative activity and inhibited lipid peroxidation significantly: In active fractions, we isolated rutin, hyperin, quercitrin and quercetin.

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Total Synthesis of New Apicidin Derivatives as Potent Antitumor Agents

  • kim, hyung-Kyo;Jin, Cheng-Hua;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.188.1-188.1
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    • 2003
  • The antiparasitic agent apicidin, which was recently isolated from cultures of Fusarium Pallidoroseum, belongs to a rare group of cyclictetrapeptide fungal metabolites. Apicidin inhibits protozoal HDAC and is orally active against Plasmodium berghei malaria in mice. The biological activity of apicidin appears to be attributable to inhibition of apicomplexan HDAC at low nanomolar concentrations. In the present, we have worked about the synthesis of new apicidin derivatives and discovered that apicidin and some derivatives have mild antitumor activity. (omiited)

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Pharmacodynamics of anticancer activity of tirapazamine and paclitaxel against human NSCLC

  • Park, Jong-Kook;Kang, Jin-Hyoung;Kuh, Hyo-Jeong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.228.1-228.1
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    • 2002
  • Hypoxia in solid tumors is known to contribute to intrinsic chemoresistance. Tirapazamine(TPZ). a hypoxia-selective cytotoxin. showed synergism with radiation or cytotoxic agents. Paclitaxel(PTX) is a highly active anti-cancer agent against Non small cell lung cancer(NSCLC), however. due to poor penetration into central hypoxic region of tumor tissue. combination with TPZ has been suggested to enhance its efficacy. (omitted)

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Flexible docking of novel antitumor agents into human topoisomerase I-DNA complex with FlexiDock

  • Woo , Su-Na;Kim, Choon-Mi
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.314.2-314.2
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    • 2002
  • DNA topoisomerases catalyze changes in DNA topology through cycles of transient DNA strand breakage and religation. During this process. the active site tyrosine in human DNA topoisomerase Ⅰ(Top Ⅰ) becomes covalently linked to the 3'-ends of a single-stranded nick in the DNA duplex, Stabilization of the Top Ⅰ-DNA cleavable complex is the common initial event leading to the cytotoxicity of top 1 inhibitors. (omitted)

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Studies on the Pharmacologically Active Substances of Pursatilla koreana -The Isolation of Hederagenin- (Pursatilla koreana의 약효성분 ( I ) -Hederagenin의 분리-)

  • Kim, Il-Hyuk;Kim, Ki-Ho
    • Korean Journal of Pharmacognosy
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    • v.2 no.3
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    • pp.121-123
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    • 1971
  • In series of the the development of domestic natural products, the studies were conducted to evaluate the pharmacologically active substances of the roots of Pursatilla koreana, which is a specific plant, widely distributed in this country and known to be effective as antiinflammatory, hemostatic and antidysentric agents in oriental remedies. From the hydrolysis of methanol extract of the root, a triterpenic substance was isolated. It was identified as $hederagenin\;C_{30}H_{48}O_4,\; m.p.\;333^{\circ}{\sim}334^{\circ}$, by the m.m.p. with authentic sample, elemental analysis, IR, mass spectra and the other physico-chemical experimentations.

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