• Title/Summary/Keyword: Analogs

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Pharmacophore Modelling, Quantitative Structure Activity Relationship (QSAR) and Docking Studies of Pyrimidine Analogs as Potential Calcium Channel Blockers

  • Choudhari, Prafulla B.;Bhatia, Manish S.;Jadhav, Swapnil D.
    • Journal of the Korean Chemical Society
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    • v.57 no.1
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    • pp.99-103
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    • 2013
  • The present communication deals with the Pharmacophore modeling, 3D QSAR and docking analysis on series of Pyrimidine derivatives as potential calcium channel blockers. The computational studies showed hydrogen bond donor, hydrogen bond acceptor, and hydrophobic group are important features for calcium channel blocking activity. These studies showed that Pyrimidine scaffold can be utilized for designing of novel calcium channels blockers for CVS disorders.

Minimum Hellinger Distance Bsed Goodness-of-fit Tests in Normal Models: Empirical Approach

  • Dong Bin Jeong
    • Communications for Statistical Applications and Methods
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    • v.6 no.3
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    • pp.967-976
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    • 1999
  • In this paper we study the Hellinger distance based goodness-of-fit tests that are analogs of likelihood ratio tests. The minimum Hellinger distance estimator (MHDE) in normal models provides an excellent robust alternative to the usual maximum likelihood estimator. Our simulation results show that the Hellinger deviance test (Simpson 1989) based goodness-of-fit test is robust when data contain outliers. The proposed hellinger deviance test(Simpson 1989) is a more direcct method for obtaining robust inferences than an automated outlier screen method used before the likelihood ratio test data analysis.

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Comparative Vibrational Spectroscopic Studies Between Nickel, Zinc Tetraphenylporphyrins and Tetraphenylchlorins

  • Song Ok-Keun;Yoon Min-Joong;Chang Jae-Rim;Kim Dongho
    • Bulletin of the Korean Chemical Society
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    • v.10 no.1
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    • pp.39-51
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    • 1989
  • The infrared and resonance Raman spectra are reported for nickel and zinc tetraphenylchlorins. It is found that the IR and RR spectra become more complicated compared with the corresponding porphyrin analogs due to the symmetry changes. Some vibrational parameters like the core size and the symmetry change are examined in accordance with vibrational spectra of other type of chlorins.

An Efficient and Eco-friendly Approach to $^15N-Unsubstituted {\beta}-Lactams: ^15-Labled$ Synthons for Taxol and Its Analoss

  • Park, Sang Hyeon;Lee, Sang Yeop
    • Bulletin of the Korean Chemical Society
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    • v.22 no.5
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    • pp.493-498
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    • 2001
  • An efficient and eco-friendly approach to N-unsubstituted ${\beta}-lactams$ has been developed using mostly water as the reaction medium. This methodology was applied to the synthesis of N-unsubstituted 3-hydroxy-4-phenyl-2-azetidinone derivatives (inclu ding 15N-labeled version) which are suitable precursors for the C-13 side chain of taxol and its analogs.

The principles of posionous mushrooms, their unexpected utilitie

  • Shirahama, Hirushisa
    • Plant Resources
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    • v.3 no.1
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    • pp.100-104
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    • 2000
  • Lampteromyces japonicus is the most popular source of mushroom poisoning in Japan. We isolated poisonous substance, illudin S, 40 years ago, which shower strong anti-tumoric activity. Its analogs are now the most hopeful anti-cancer agent. Clitocybe acromelalgia gives unique poisoning which exhibits symptoms similar to acromelalgia and erythromelalgia. We intended to isolate the toxin causing these poisoning but neuroexciatory compounds, acromelic acids A and B, were isolated. They are now known as the most potent glutamate agonists and good reagents for the study of the glutamate receptor of a neurocell.

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Synthesis of 4-Aza-cholestane Derivatives Containing Nitrosoureido Function as Antitumor Activity

  • Kim, Jack C.;Park, Jin Il;Hur, Tae-Ho
    • Bulletin of the Korean Chemical Society
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    • v.14 no.2
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    • pp.176-178
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    • 1993
  • A series of 4-(2-chloroethyl)nitrosocarbamoyl- and 4-methyl nitrosocarbamoyl analogs of 4-Aza-$5{\alpha}$-cholestane (5a and 5b), 4-Aza-5-cholestene (6a and 6b) were synthesized and evaluated for their inhibitory activity against the Sarcoma 180 cell. The steroidal nitrosoureas, 5a, 5b, 6a and 6b displayed modest activity in vitro.

Synthetic beta-Lactam Antibiotics I. Synthesis and Antibacterial Activity of 7-Amino-3-[1-(halo-substituted phenyl)-1H-tetrazole-5-yl]thiomethyl-3-cepheme-4-carboxylic acids

  • Koh, Dong-Soo;Park, Sang-Woo;Kim, You-Seung
    • Bulletin of the Korean Chemical Society
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    • v.8 no.3
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    • pp.189-192
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    • 1987
  • The syntheses of mercaptotetrazoles and cephalothin analogs are described. Their in vitro potency was established. The compounds exhibited high antibacterial activity against Gram-positive bacteria and moderate activity against Gram-negative bacteria.

Selective Cytotoxicity of Novel Platinum(II) Complexes on Gastric Cancer Cell-Lines and Normal Kidney Cells

  • Kim, Jung-Tae;Hong, Eon-Pyo;Rho, Young-Soo;Jung, Jee-Chang
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.358.3-358.3
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    • 2002
  • We recently synthesized new platinum(II) complex analogs containing trans-1 and cis-l.2-diaminocyclohexane (DACH) as carrier ligands and L -3-phenyllactic acid(PLA) as a leaving group. Our platinum-based drug discovery program has been aimed at developing drugs capable of diminishing toxicity and improving selective cytotoxicity. (omitted)

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Synthesis of thiazolidinedione analogs

  • Yun, Hyun-Jin;Cheon, Seung-Hoon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.177.2-177.2
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    • 2003
  • Thiazolidinediones (TZDs) are a new class of compound that increase insulin sensitivity in type 2 diabetic patients. Thiazolidinediones (TZDs) act as ligands for a member of the nuclear hormone receptor superfamily, peroxisome proliferator-activated receptor-$\gamma$ (PPAR-$\gamma$), which is highly expressed in fatty tissue and, moreover, has been shown to play an important role in fat cell differentiation. The strong interaction between the antidiabetic activity ofTZDs and their ability to activate PPAR-$\gamma$ suggests that PPAR-$\gamma$, through downstream-regulated genes, mediates the effects of TZDs. (omitted)

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