• Title/Summary/Keyword: Analogs

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The Role of Substituents of ar-Turmerone for its Anticancer Activity

  • Oh, Won-Geun;Baik, Kyong-Up;Jung, Sang-Hun;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.15 no.3
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    • pp.256-262
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    • 1992
  • For the evaluation of the role of substituents of ar-turmerone for its anticancer activity, ar-turmerone (1a) and its analogs like 2-methyl-6-(4'-methyphenyl)-2-octen-4-one (1b), 2-methyl-6-phenyl-2-hepten-4-one (1c), 2-methyl-6-phenyl-2-octen-4-one (1d) and 2 methyl-6-(trans-4'-methylcyclohexyl)-2-hepten-4-one (1e) were preparedd and their cytotoxic activities against $L_{1210}$ cell were determined. Omission of methyl group at para-position dose not variate the cytotoxicity of ar-turmerone. Elongation of alkyl group at 6-position decreases $ED_{50}$ value. Saturation of aromatic ring of ar-turmerone markedly decreases the cytotoxicity. Therefore the smaller size of alkyl group at 6-position and aromatic ring of ar-turmerone should be essential for exhibiting its anticancer activity.

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COVERING AND INTERSECTION CONDITIONS FOR PRIME IDEALS

  • Chang, Gyu Whan;Hwang, Chul Ju
    • Korean Journal of Mathematics
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    • v.17 no.1
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    • pp.15-23
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    • 2009
  • Let D be an integral domain, P be a nonzero prime ideal of D, $\{P_{\alpha}{\mid}{\alpha}{\in}{\mathcal{A}}\}$ be a nonempty set of prime ideals of D, and $\{I_{\beta}{\mid}{\beta}{\in}{\mathcal{B}}\}$ be a nonempty family of ideals of D with ${\cap}_{{\beta}{\in}{\mathcal{B}}}I_{\beta}{\neq}(0)$. Consider the following conditions: (i) If $P{\subseteq}{\cup}_{{\alpha}{\in}{\mathcal{A}}}P_{\alpha}$, then $P=P_{\alpha}$ for some ${\alpha}{\in}{\mathcal{A}}$; (ii) If ${\cap}_{{\beta}{\in}{\mathcal{B}}}I_{\beta}{\subseteq}P$, then $I_{\beta}{\subseteq}P$ for some ${\beta}{\in}{\mathcal{B}}$. In this paper, we prove that D satisfies $(i){\Leftrightarrow}D$ is a generalized weakly factorial domain of ${\dim}(D)=1{\Rightarrow}D$ satisfies $(ii){\Leftrightarrow}D$ is a weakly Krull domain of dim(D) = 1. We also study the t-operation analogs of (i) and (ii).

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Synthesis of Water Soluble Analogs of Arylsulfonylimidazolidinone (JSH-2282)

  • Bang, Seong-Cheol;Lee, Ki-Cheul;Sharma, Vinay K.;Sharma, Niti;Yang, Hyun-Sun;Jung, Sang-Hun
    • Bulletin of the Korean Chemical Society
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    • v.34 no.7
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    • pp.2011-2015
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    • 2013
  • To improve the water solubility of arylsulfonylimidazolidinone (JSH-2282), a potent anti-cancer agent, two urea derivatives, sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)-phenyl)ureido)succinate (2a) and sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)phenyl)ureido)pentanedioate (2b), were synthesized and studied for solubility and anti-cancer activity.

Synthesis and Evaluation of Molecularly Imprinted Polymeric Microspheres for Chloramphenicol by Aqueous Suspension Polymerization as a High Performance Liquid Chromatography Stationary Phase

  • Zhang, Yan;Lei, Jiandu
    • Bulletin of the Korean Chemical Society
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    • v.34 no.6
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    • pp.1839-1844
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    • 2013
  • Molecularly imprinted microsphere for chloramphenicol (CAP) with high adsorption capacity and excellent selectivity is prepared by aqueous suspension polymerization, in which chloramphenicol is used as template molecule and ethyl acetate as porogen. The CAP-imprinted microspheres are used as high performance liquid chromatography (HPLC) stationary phase and packed into stainless steel column ($150mm{\times}4.6mm$ i.d.) for selective separation of chloramphenicol. HPLC analysis suggests that chloramphenicol can be distinguished from not only its structural analogs but also other broad-spectrum antibiotic such as erythromycin and tetracycline. In addition, the binding experiments of CAP-imprinted microspheres are carried out in ethanol/water (1:4, V:V), the results indicate that the maximum apparent static binding capacity of molecularly imprinted microspheres is up to 66.64 mg $g^{-1}$ according to scatchard model.

Fungicidal activity of synthetic piericidin analogs as inhibitors of NADH-ubiquinone oxidoreductase on the respiratory chain (호습쇄의 NADH-ubiquinone oxidoreductase 저해제인 합성 piericidin유사체드르이 살균활성)

  • Chung, Kun-Hoe;Cho, Kwang-Yun;Takahashi, Nobutaka;Yoshida, Shigeo
    • Applied Biological Chemistry
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    • v.33 no.3
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    • pp.264-267
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    • 1990
  • Representative synthetic piericidin-like compounds, such as hydroxypyridine and hydroxyquinoline derivatives, which showed high inhibition activity against NADH-ubiquinone oxidoreductase on the respiratory chain revealed good fungicide activity. Especially, hydrolrypyridine ones showed high activity against rice blast (Pyricularia oryzae) and barley powdery mildew (Erysiphe graminis).

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Synthesis and Photoaffinity Labeling of 3'(2')-O-(p-azidobenzoyl) ATP

  • Shin, Seung-Jin;Lee, Woo-Kyoung;Park, Jong-Sang
    • BMB Reports
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    • v.30 no.3
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    • pp.211-215
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    • 1997
  • A photoactive analog of ATP, 3'(2')-O-(p-azidobenzoyl)-adenosine 5-triphosphate (AB-ATP) was synthesized by chemically coupling N-hydroxysuccinimidyl-4-azidobenzoate (NHS-AB) and ATP. The utility of AB-ATP as an effective active-site-directed photoprobe was demonstrated using catalytic subunit of protein kinase A as a model enzyme. Photoincorporation of AB-ATP was saturated with apparent dissociation constant of $30{\mu}m$ and protected completely by $100{\mu}m$ of ATP. When the enzyme was covalently modified by photolysis in the presence of saturating amounts of photoprobe, about 60% inhibition of enzyme activity was observed. These results demonstrate that AB-ATP has potential application as a probe to characterize ATP-binding proteins including protein kinases.

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3D QSAR (3 Dimensional Structure Activity Relationship) Study of Mutagen X

  • Yoon, Hae-Seok;Cho, Seung-Joo
    • Molecular & Cellular Toxicology
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    • v.1 no.1
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    • pp.46-51
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    • 2005
  • Mutagen X (MX) exists in our drinking water as the bi-products of chlorine disinfection. Being one of the most potent mutagen, it attracted much attention from many researchers. MX and its analogs are tested and modeled by quantitative structure activity relationship (QSAR) methods. As a result, factors affecting this class of compounds have been found to be steric and electrostatic effects. We tried to collect all the data available from the literature. The quantitative structure-activity relationship of a set of 29 MX was analyzed using Molecular Field Analysis (MFA) and Receptor Surface Analysis (RSA). The best models gave $q^{2}=0.918,\;r^{2}=0.949$ for MFA and $q^{2}=0.893,\;r^{2}=0.954$ for RSA. The models indicate that an electronegative group at C6 position of the furanone ring increases mutagenicity.

Isoquinolines: Are they possible candidate for $Ca^{2+}$ blockers\ulcorner

  • 장기철;윤용진;조수동;정원석
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.217-217
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    • 1994
  • Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

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Foods and functional foods containing mushroom, mushroom extracts, and mushroom-derived compounds (버섯원물과 버섯 추출물 그리고 버섯 유래 화합물을 포함한 식품과 기능성식품)

  • Jo, Han-Gyo;Shin, Hyun-Jae
    • Journal of Mushroom
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    • v.15 no.4
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    • pp.155-163
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    • 2017
  • Mushrooms and their extracts including purified ingredients, are currently used as foods, functional foods (and/or nutraceuticals), and medicines. These products have numerous bioactive compounds such as polysaccharides (mainly ${\beta}$-glucans), glycoproteins, nucleotide analogs, terpenoids, and polyphenols, which have exhibited antioxidant, antimicrobial, anticancer, antiviral, anti-obesity, and immunomodulatory activities. In this review, we discuss the current information on the biactivities of 10 popular mushrooms in Korea. We also summarize the information on mushrooms and the active compounds derived from them, as well as mushroom-based products such as foods, functional foods, and medicines. We believe this review could provide useful information for scientists and consumers who seek to develop new products and promote healthy food habits and lifestyle.

Synthesis and biological activity of spirobenzopyranone derivative as analogs of thelepin, isolated from the marine annelid Thelepus setosus (항균성물질 thelepin의 spirobenzopyranone 유도체의 합성과 생물활성)

  • Ko, Byoung-Seob;Oritani, Takayuki
    • Applied Biological Chemistry
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    • v.35 no.6
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    • pp.470-474
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    • 1992
  • For the further development of thelepin analog as antibiotic agents, we undertook the synthesis of spirobenzopyranone derivative ${\underline{5}}$ as thelepin analog by oxidative phenol coupling. The spirobenzopyranone analog ${\underline{5}}$ showed high activity against Bacillus subtilis (IFO 3108) in $5\;{\mu}g/disc$.

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