• Title/Summary/Keyword: Active compounds

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Synthesis of Novel Allylthio Heterocyclo(or aryl)alkylaminopyridazines and Their Anticancer Activity against SK-Hep-1 Cells

  • Lee, Myung-Sook;Kim, Eun-Sook;Moon, A-Ree;Park, Myung-Sook
    • Bulletin of the Korean Chemical Society
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    • v.30 no.1
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    • pp.83-91
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    • 2009
  • To develop new anticancer agents, 3-allylthio-6-aminopyridazine derivatives were synthesized from maleic anhydrides or phthalic anhydrides by formation of a pyridazine nucleus, dichlorination, allylthiolation and amination. The pyridazine nuclei were obtained by condensing a hydrazine monohydrate with maleic anhydride. An allylthio group as a pharmacologically active group was introduced into one side of a pyridazine ring. Arylalkylamines with benzene or pyridine moieties or heterocycloalkylamines with heterocycle moieties such as morpholine, piperidine, or pyrrolidine were also introduced into the para-position of allylthio pyridazine. These new compounds showed antiproliferative activities against SK-Hep-1 human liver cancer cells in MTT assays. These compounds are thus promising candidates for chemotherapy of hepatocellular carcinomas. Two compounds, 20c and 22a, showed higher potencies for inhibiting growth of hepatocellular carcinoma cells than did K6 ($ID_50$=1.08 mM). This suggests the potential anticancer activity of these two compounds.

Design. Synthesis and Antitumor Evaluation of Terpyridine Derivatives Containing Pyridines at 4'- Position

  • Lim, Hyun-Tae;Moon, Yoon-Soo;Zhao, Longxuan;Kim, Eun-Kyung;Kim, Tae-Hyung;Lee, Eung-Seok
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.347.3-347.3
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    • 2002
  • Recent study indicated that terpyridine and its derivatives displayed highly active antitumor properties. In this presentation. derivatives of terpyridines having three pyridine moieties at 2',4',6'-position of central pyridine skeleton were prepared, and evaluated their cytotoxicity against several human cancer cell lines and topoisomerase I inhibitory activities. Most of the prepared compounds showed strong cytotoxicity compared to doxorubicln. In addition. several compounds displayed better cytotoxicity than that of doxorubicin. In addition, several compounds displayed better cytotoxicity than that of doxorubicin. Structure-activity relationship study was perfomed to be indicated that [2.2':6',2']terpyidine skeleton is important to show strong xytotoxicity. Significant topoxicity. Significant topoisomerase I inhibitory activity was not observed for prepared compounds.

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Overview of active packaging to maintain the quality of fresh food products - focusing on controlled release packaging (식품의 선도 유지를 위한 액티브 포장 연구 고찰 기능성 방출 조절 포장 중심)

  • Lee, Myung-Ho;Lee, Youn Suk
    • Food Science and Industry
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    • v.50 no.2
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    • pp.27-36
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    • 2017
  • Today, the food packaging industry has a great interest in using active packaging to fresh food product as a solution for the future to positively provide its quality, safety and shelf life. Many researches have extensively studied functional packaging strategies in recently years. Controlled release packaging (CRP) is an innovative packaging technology in the packaging polymer matrix from which can active agents are delivered in a controlled way into the product. CRP technology is well-suited for controlling release of antimicrobial compounds and antioxidants to prevent food degradation reactions such as microbial growth and lipid oxidation. Advances in CRP technology allow food packaging manufacturers to challenge the development of better functional food packaging systems. This overview examines the most recent developments and technologies of active packaging for applying the food industry. The scope of this article has mainly been focused on controlled releasing systems.

Bioactive Fabaceous Saponins and Structure-Activity Relationship

  • Kinjo, Junei;Nohara, Toshihiro
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.143-146
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    • 2002
  • Saponins are glycosidic compounds present in many edible and inedible plants. Structurally, they are composed of a lipid-soluble aglycone consisting of either a sterol or, more commonly, a triterpenoid and water-soluble sugar residues differing in type and amount of sugars [1]. Because of their amphiphilic nature, they are highly surface-active. Their biological activity is closely related to the chemical structures that determine the polarity, hydrophobicith and acidity of compounds [1]. (omitted)

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Reactions with Hydrazidoyl Halides (V): Synthesis of Some Amidrazones, Hydrazides, Pyrazoles and Pyrazolo [3, 4-d] pyridazine Derivatives

  • Attaby, Fawzy A.;Zaki, Mayssoune Y.;Abdelhamid, Abdou O.;Ramadan, Nazmy A.
    • Archives of Pharmacal Research
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    • v.13 no.4
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    • pp.314-318
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    • 1990
  • 2-Bromo (2'-benzofury)gloxal-2-aryhydrazones I reacted with nucleophiles displacing the bromide. Treatment of I with active methylene compounds yield the pyrazole derivatives VIII-XI. Compounds XII-XIV reacted with hydrazine to give pyrazolo (3, 4-dipyridazine derivative XIV-XIV. The structures of the products were assigned and confirmed on the basis of their elemental analysis and spectral data.

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Synthesis of Yakuchinone Derivatives and Their Inhibitory Activities on Nitric Oxide Synthesis (Yakuchinone과 그 유도체의 합성 및 Nitric Oxide생성 저해효능)

  • 윤정화;안한나;류재하;김희두
    • YAKHAK HOEJI
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    • v.45 no.1
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    • pp.16-22
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    • 2001
  • Novel yakuchinone derivatives have been designed, synthesized and evaluated their inhibitory activity of NO production in lipopolysaccharide (LPS)-activated macrophages. From this study, some enone compounds have been found to be highly active in the assay. In view of the importance of NO in septic shock and inflammation, these compounds may be useful candidates for the development of new drug to treat endotoxemia and inflammation accompanying overproduction of NO.

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Asymmetric Synthesis in Pharmaceutical Manufacturing Chemistry

  • Jew, Sang-Sup
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.59-61
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    • 2003
  • Organic compounds play an important role in the area of pharmaceutical, agrochemical, and other materials, which possess useful biological activities. Generally, such biological activities are come from the interaction of the organic compounds with the receptors in biological system, such as enzymes. Such receptors are composed of the chiral building blocks such as amino acid or carbohydrate, which means the biological active sites of receptors are chiral. (omiited)

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Screening for Natural Bioactive Compounds Targeting the Intracellular Signal Transduction Pathway: Natural Products Modulating the Expression of the Interleukin-2 gene

  • Hakamatsuka, Takashi
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.60-61
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    • 2003
  • Human Genome Project has recently been completed and the information on nucleotide sequences of our whole genome is now available at the public or commercial data banks. Next goals are to identify the functions of each gene and to elucidate the intracellular signal transduction pathways regulating gene expression. We have established a PCR-based bioassay to search for biologically active compounds that can modulate the expression of genes encoding important proteins. (omitted)

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Developing a pharmacophore model for nonpeptide bradykinin antagonists

  • Park, Hae-Young;Choi, Su-Young;Lee, Su-Jin;Koh, Hune-Yeong;Pae, Ae-Nim
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.176.1-176.1
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    • 2003
  • Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. To understand the structural basis for the bradykinin antagonistic activity and to guide the design of more potent compounds we analysed the three dimensional pharmacophore model. Seven active compounds very recently reported such as FR 167344, FR 173657, LF 160687, and bradyzide were used as our pharmacophore model analysis. (omitted)

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The 3D-QSAR study of non-peptide bradykinin antagonists by CoMFA

  • Park, Hea-Young;Choi, Su-Young;Lee, Su-Jin;Kam, Yu-Rim
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.186.1-186.1
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    • 2003
  • Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. Some active compounds such as FR 173657, LF 160687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed and synthesized the iminodiacetic acid derivatives having two or three amide bonds and lipophilic ring system in each molecule. Liquid phase combinatorial synthesis using the iminodiacetic acid template gave diverse individual compounds rapidly and efficiently on a 10-50 mg scale. (omitted)

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