• Archives of Pharmacal Research
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• v.25 no.5
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• pp.585-589
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• 2002

Three hairpin polyamides were designed and synthesized by a haloform reaction and DCC/HOBt coupling reaction without amino protection and deprotection. Their anticancer activity were investigated with three kinds of cell lines-hepatic carcinoma, lung carcinoma and gastric carcinoma, and the values of $IC_{50}$ were at range of $10^{-7}~10^{-8}M$.

• YAKHAK HOEJI
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• v.42 no.1
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• pp.12-24
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• 1998

For the development of new cephalosporin antibiotics with aminothiazolcarboxymethylethoxyimino moiety on the C-7 position and tetrazolymethyl moiety on the C-3 position of cephe m ring, 7${\beta}$-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(substituted)tetrazol-2-yl]methyl-3-cephem-4-carboxylic acids(28-35) were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. They showed remarkable antibacterial activity against Escherichia coli AB 1157, Escherichia coli AB 0111, Escherichia coli BE 1186, Micrococcus luteus ATCC 9341, Salmonella typhimurium TV 119, Salmonella typhimurium SL 1102, Staphylococcus aureus IFO 12732, Staphylococcus aureus R-209, but these compounds were not active against Pseudomonas aeruginosa N-10.

• Journal of the Korean Chemical Society
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• v.42 no.2
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• pp.214-219
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• 1998

Dynorphin B analogues, $[Arg^{11}, D-Ala^{12}]$dynorphin B, $[D-Ala^2, Ala^6, Arg^{11}, D-Ala^{12}]$dynorphin B, and dynorphin B (1-11) were synthesized by solid-phase method. A chloromethylated polystyrene resin cross-linked with 2% divinylbenzene was substituted with Thr in ethanol to contain 1.20 mmol Thr/g of resin. All amino groups of amino acids were protected with t-Boc group and 2,6-dichlorobenzyl and nitro groups were used to protect the side chains of Tyr and Arg, respectively. Stepwise synthetic method was applied for synthesis of the products. Dicyclohexylcarbodiimide (DCC) and 1-hydroxybenzotriazole (HOBT) were used as the coupling reagents. The crude peptides were purified by gel filteration on Sephadex LH-20 column $(2 \times 50 cm)$ using MeOH/MeCN (3/1) and then characterized with HPLC, amino acid analyzer.

• Bulletin of the Korean Chemical Society
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• v.32 no.6
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• pp.1891-1896
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• 2011

On the basis of potent HDAC-inhibitory activity and anticancer activity of SAHA, novel SAHA derivatives 3a-d and 7 with a bulky cap such as p-dimethylaminophenyl, 4-phenylaminophenyl, 4-phenyloxyphenyl, 9H-fluorenyl or naphthalenyl ring were synthesized starting from the corresponding aryl amines or naphthalenyl acetic acid using an EDC-mediated amide coupling reaction in the presence of HOBt followed by a nucleophilic addition-elimination reaction with hydroxylamine. Compounds 3b, 3c and 3d showed more potent inhibitory activity on total HDACs (14~27-fold), HDAC1 (8~15-fold), HDAC2 (1.3~25-fold) and HDAC7 (1~3-fold) and more potent anticancer activity (2~22-fold) against MCF-7, MDA-MB-231, MCF-7/Dox, MCF-7/Tam, SK-OV-3, LNCaP and PC3 human cancer cell lines than SAHA.

• Journal of the Korean Chemical Society
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• v.64 no.2
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• pp.79-83
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• 2020

A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC₅₀) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC₅₀), cytotoxicity concentration (CC₅₀) and in vitro efficacy index (iEI), 6 (IC₅₀ = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC₅₀ = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.