• 제목/요약/키워드: Combinatorial Chemistry

검색결과 62건 처리시간 0.026초

Facile Synthesis of 3-Thioxo-3H-benzo[f]chromen-2-yl methanone and 3H-Benzo[f]chromene-3-one Under Solvent Free Condition

  • Singh, Okram Mukherjee;Devi, Nepram Sushuma;Devi, Laishram Ronibala;Lim, Ki-Bum;Yoon, Yong-Jin;Lee, Sang-Geyong
    • Bulletin of the Korean Chemical Society
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    • 제32권1호
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    • pp.175-178
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    • 2011
  • A facile, convenient, efficient and high yielding synthesis of a combinatorial library of coumarins has been developed by the condensation of readily available $\beta$-oxodithioesters and S,S-acetal with 2-hydroxy-1-naphthaldehyde in the presence of catalytic amount of $CuCl_2$ under solvent free conditions.

SrAl2O4(Eu,Dy,Nd) 압광체를 이용한 균열첨단에서의 응력장 가시화 연구 (Direct Observation of Crack Tip Stress Field Using the Mechanoluminescence of SrAl2O4:(Eu,Dy,Nd))

  • 김지식;손기선
    • 소성∙가공
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    • 제12권5호
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    • pp.493-497
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    • 2003
  • The present investigation aims at visualizing the crack tip stress field using a mechanoluminescence material. The well known compound $SrAl_2O_4$:$Eu^{2+}$ was adopted as a mechanolurninescence material. Two more trivalent rare-earth elements such as Dy and Nd were taken into consideration as codopants to provide the appropriate trap levels. Samples of a variety of compositions were prepared by varing $Eu^{2+}$, $Dy^{3+}$, and $Nd^{3+}$ doping contents, for which the combinatorial chemistry method was used. In order to search for the optimum composition for the highest mechanoluminescence, the luminescence induced by a compressive device including a CCD camera. In parallel, a compact tension specimen was prepared by mixing the luminescence powders of optimum composition and epoxy resin. Crack initiation from the mechanically machined sharp note tip and its growth during loading were found to be associated with the extent of light emission from $SrAl_2O_4$.

Combinatorial Fine-Tuning of Phospholipase D Expression by Bacillus subtilis WB600 for the Production of Phosphatidylserine

  • Huang, Tingting;Lv, Xueqin;Li, Jianghua;Shin, Hyun-dong;Du, Guocheng;Liu, Long
    • Journal of Microbiology and Biotechnology
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    • 제28권12호
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    • pp.2046-2056
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    • 2018
  • Phospholipase D has great commercial value due to its transphosphatidylation products that can be used in the food and medicine industries. In order to construct a strain for use in the production of PLD, we employed a series of combinatorial strategies to increase PLD expression in Bacillus subtilis WB600. These strategies included screening of signal peptides, selection of different plasmids, and optimization of the sequences of the ribosome-binding site (RBS) and the spacer region. We found that using the signal peptide amyE results in the highest extracellular PLD activity (11.3 U/ml) and in a PLD expression level 5.27-fold higher than when the endogenous signal peptide is used. Furthermore, the strain harboring the recombinant expression plasmid pMA0911-PLD-amyE-his produced PLD with activity enhanced by 69.03% (19.1 U/ml). We then used the online tool \RBS Calculator v2.0 to optimize the sequences of the RBS and the spacer. Using the optimized sequences resulted in an increase in the enzyme activity by about 26.7% (24.2 U/ml). In addition, we found through a transfer experiment that the retention rate of the recombinant plasmid after 5 generations was still 100%. The final product, phosphatidylserine (PS), was successfully detected, with transphosphatidylation selectivity at 74.6%. This is similar to the values for the original producer.

High Temperature Size Exclusion Chromatography for High Throughput Analysis

  • Chang, Tai-Hyun;Park, Soo-Jin;Cho, Hee-Sook;Kim, Young-Tak;Ihm, Kyu-Hyun
    • 한국고분자학회:학술대회논문집
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    • 한국고분자학회 2006년도 IUPAC International Symposium on Advanced Polymers for Emerging Technologies
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    • pp.202-202
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    • 2006
  • With a modern size exclusion chromatography (SEC) column, molecular weight analysis of a polymer sample takes about 10 min. However, it is desirable to reduce the analysis time further, in particular, for high throughput measurements required in combinatorial analyses or 2D-HPLC analyses. We implemented the high temperature SEC for the purpose. By inserting a narrow bore tubing between the column and the detector, a sufficient backpressure can be maintained to prevent the mobile phase from boiling and the effluent is cooled down enough when it reaches the detector. Therefore, a normal SEC detector can be used without any modification. The SEC resolution is greatly improved at the elevated temperature at high flow rate which allows high speed operation.

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Screening for bioactive compounds from natural products by ELISA assay

  • Iwanami, Naoko
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.34-37
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    • 1998
  • Combinatorial chemistry is one of the most interested topics in the area of drug discovery. One of the most important points is how to find a lead compound that gives the seed structure for designing of a combinatorial library. Natural products is suitable for searching a new bioactive compound with new structure. We have carried out systematic screening works to find natural products possessing the effects on inter-and intra-cellular signaling. Two hundreds extracts of medical plants and two thousands microbial culture broth samples have been tested for the induction and inhibition of IL-2 or IL-6 production (Fig. 1). ELISA is an efficient method for screenings from such a large number of samples. Now, we apply this method to search prion- binding agents.

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Investigation of Angiotensin Glycosylation by MALDI-TOF and ESI Tandem Mass Spectrometry

  • Park, Soo-Jin;Park, Deok-Hie;Sul, Soo-Hwan;Oh, Sung-Hwan F.;Park, In-Sook;Chung, Doo-Soo;Kim, Hie-Joon;Kim, Min-Sik;Lee, Sang-Won
    • Bulletin of the Korean Chemical Society
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    • 제25권12호
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    • pp.1791-1800
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    • 2004
  • Angiotensin I, a model decapeptide, was glycosylated and partially hydrolyzed with HCl (6 N, 80 $^{\circ}C$, 4 h), aminopeptidase, and carboxypeptidase Y. A single peptide mass map obtained from truncated peptides in the partial acid hydrolysate of angiotensin and its glycosylation product mixture by matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry enabled sequencing of angiotensin by a combinatorial procedure. MALDI-TOF and electrospray ionization (ESI) tandem mass spectrometric results indicate that both the N-terminal amino group of aspartic acid and the guanidinium group of the second residue arginine are glycosylated.

A Carbazole Based Bimodal "Turn-On" Fluorescent Probe for Biothiols (Cysteine/Homocysteine) and Fluoride: Sensing, Imaging and its Applications

  • Kaur, Matinder;Yoon, Byungkwon;Kumar, Rajesh;Cho, Min Ju;Kim, Hak Joong;Kim, Jong Seung;Choi, Dong Hoon
    • Bulletin of the Korean Chemical Society
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    • 제35권12호
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    • pp.3437-3442
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    • 2014
  • A well-known carbazole-based precursor (probe 1) was used for the detection of cysteine/homocysteine and fluoride. Probe 1 shows a "turn-on" response to cysteine/homocysteine and fluoride via enhancement in emission intensity at 442 nm and 462 nm respectively, in solutions and living cells. Furthermore, probe 1 behaves as a fluorescent molecular switch between cysteine/homocysteine and fluoride as the chemical inputs, which have been used for the development of a combinatorial logic circuit and a molecular keypad lock.

Natural Modulators of Estrogen Biosynthesis and Function as Chemopreventive Agents

  • Bhat, Krishna P.L.;Pezzuto, John M.
    • Archives of Pharmacal Research
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    • 제24권6호
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    • pp.473-484
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    • 2001
  • There is clearly a need for novel breast cancer chemopreventive agents with enhanced potency and specificity with tittle or no side effects. To this end, several new chemical moieties have been synthesized or isolated from natural sources. In this reviewal we have described some agents currently in use or under development for treatment or prevention of breast cancer, as well as our own strategies for the discovery of natural product modulators of estrogen biosynthesis and function. In particulars bioassay-guided fractionation of active plant extracts is a unique method for identifying agents with novel mechanisms of action, some of which should be useful for prevention of human cancer. Further, with the advent of combinatorial chemistry and high throughput screening, even greater progress may now be expected with natural product leads.

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An Efficient Synthesis of α-Amino-δ-valerolactones by the Ugi Five-Center Three-Component Reaction

  • Kim, Young-Bae;Park, Soo-Jung;Geum, Gyo-Chang;Jang, Min-Seok;Kang, Soon-Bang;Lee, Duck-Hyung;Kim, You-Seung
    • Bulletin of the Korean Chemical Society
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    • 제23권9호
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    • pp.1277-1320
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    • 2002
  • A novel approach to ${\alpha}-amino-{\delta}-valerolactone$ derivatives 8 by the intramolecular Ugi five-center three-component reaction (U-5C-3CR) using the multifunctional starting material, L-pentahomoserine 5 is described.

Establishment of new cytotoxicity screening system using Caco-2 cells

  • Seok, Ji-Eun;Kim, Ki-Hwan;Kim, Dong-Chool
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.92-93
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    • 2002
  • With the recent development of combinatorial chemistry, recombinant biotechnology and rational drug design, millions of compounds are being produced in the laboratories of pharmaceutical companies. These new drug candidates are evaluated their efficacy and toxicity through in vivo animal model studies which is very important in drug development. From these studies, very successful drug candidates are selected. (omitted)

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