• Journal of the Korean Chemical Society
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• v.50 no.3
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• pp.269-271
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• 2006

• Bulletin of the Korean Chemical Society
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• v.33 no.1
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• pp.128-136
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• 2012

We report the solid-phase library construction of 222 number of a novel N-[alkyl sulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B derivatives. The polymer-bound N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 9 and amine 10 derivatives were obtained by first diversity generation with various acid chlorides and alkyl halides. Further reactions on the resins 9 and 10 with substituted sulfonyl chlorides produced the desired N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B analogues.

• Proceedings of the Korean Society of Plant Pathology Conference
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• 2003.10a
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• pp.108.1-108
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• 2003

Soil metagenome is untapped total microbial genome including that of the majority of unculturable bacteria present in soil. We constructed soil metagenomic library in Escherichia coli using DNA directly extracted from two different soils, pine tree rhizosphere soil and forest topsoil. Metagenomic libraries constructed from pine tree rhizosphere soil and forest topsoil consisted of approximately 33,700 clones and 112,000 clones with average insert DNA size of 35-kb, respectively. Subsequently, we screened the libraries to select clones with antimicrobial activities against Saccharomyces cerevisiae and Agrobacterium tumefaciens using double agar layer method. So far, we have a clone active against S. cerevisiae and a clone active against A. tumefaciens from the forest topsoil library. In vitro mutagenesis and DNA sequence analysis of the antifungal clone revealed the genes involved in the biosynthesis of antimicrobial secondary metabolite. Metagenomic libraries constructed in this study would be subject to search for diverse genetic resources related with useful microbial products.

• Bulletin of the Korean Chemical Society
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• v.32 no.10
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• pp.3805-3808
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• 2011

• Bulletin of the Korean Chemical Society
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• v.35 no.8
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• pp.2385-2390
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• 2014

Novel 2,6-difuctionalized 2H-benzopyrans were synthesized and evaluated for a sphingosylphosphorylcholine(SPC) inhibitor. The synthetic 2H-benzopyrans 1c and 3a showed high potency in SPC-induced cell proliferation assay ($IC_{50}$ < 20 nM). Neither hERG $K^+$ channel binding (> $10{\mu}M$) nor CYP inhibitions (> $10{\mu}M$) were observed. Also, the simple structure-activity relationship (SAR) results were obtained from analysis of 2H-benzopyran derivatives 1-3 and the anti-SPC effect of 2H-benzopyran 1c was confirmed by a HUVEC tube formation assay.

• Bulletin of the Korean Chemical Society
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• v.35 no.12
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• pp.3609-3617
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• 2014

A series of compounds containing both 1,3,4-oxadiazole and thiohydantoin were synthesized as a promising scaffold for application in medicinal chemistry. The key step of the synthesis is a microwave-assisted cyclization of semicarbazides possessing a thiohydantoin moiety at one of the acyl termini using $POCl_3$ as a dehydrating reagent. A wide range of semicarbazides were prepared through the substitution of hydrazides with an N-acylated thiohydantoin derived from the cyclization of the corresponding isothiocyanate with an amino acid and subsequent N-acylation of the resultant thiohydrantion. Consequently, the 58 number of 1,3,4-oxadiazole derivatives having a thiohydantoin substituent were prepared in good overall yields.

• BMB Reports
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• v.38 no.5
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• pp.517-525
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• 2005

Solid phase peptide synthesis method, which was introduced by Merrifield in 1963, has spawned the concept of combinatorial chemistry. In this review, we summarize the present technologies of solid phase peptide synthesis (SPPS) that are related to combinatorial chemistry. The conventional methods of peptide library synthesis on polymer support are parallel synthesis, split and mix synthesis and reagent mixture synthesis. Combining surface chemistry with the recent technology of microelectronic semiconductor fabrication system, the peptide microarray synthesis methods on a planar solid support are developed, which leads to spatially addressable peptide library. There are two kinds of peptide microarray synthesis methodologies: pre-synthesized peptide immobilization onto a glass or membrane substrate and in situ peptide synthesis by a photolithography or the SPOT method. This review also discusses the application of peptide libraries for high-throughput bioassays, for example, peptide ligand screening for antibody or cell signaling, enzyme substrate and inhibitor screening as well as other applications.

• Bulletin of the Korean Chemical Society
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• v.29 no.2
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• pp.323-327
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• 2008

A focused library of pyrazole-based compounds was constructed towards novel transcription factor inhibitors. Complementary hydrogen bonding interaction with b-sheet peptide structures was the basis for the design of 5-amino-3-pyrazole carboxamide scaffold. From the preliminary inhibition assay against several transcription factors, compounds 7e and 8g were identified as novel lead compounds against HIF-1a and NF-AT transcription factors, respectively.

• Bulletin of the Korean Chemical Society
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• v.32 no.10
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• pp.3752-3755
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• 2011

• KLA journal
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• v.19 no.2
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• pp.25-30
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• 1978