• Bulletin of the Korean Chemical Society
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• 제34권7호
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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.

• Bulletin of the Korean Chemical Society
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• 제32권12호
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• pp.4309-4315
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• 2011

For synthesis of benzastatin E, F and G analogues, the indole-2-carbaldehydes with or without substituents at C-5 position were prepared as key intermediates. Several synthetic attempts to achieve benzastatin E-G analogues were suggested using the indole-2-carbaldehyde intermediates.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.142-150
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• 2005

The synthesis and structure-activity relationships of a novel series of substituted quercetins that activates peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) are reported. The $PPAR{\gamma}$ agonistic activity of the most potent compound in this series is comparable to that of the thiazolidinedione-based antidiabetic drugs currently in clinical use.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.217.1-217.1
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• 2003

Phytoestrogen has been used as supplement in order to treat osteoporosis. The representative phytoestrogen, isoflavones, are daidzein, genistein and formononetin which were present highly in legumes. We have studied the quantitative analysis of isoflavones in KUNBO by HPLC. KUNBO, a mixed herbal extract including Astragali Radix and Rhynchosiae nulubilis Semen (Leguminosae), etc., is a nutraceutical candidate for type I osteoporosis. olumn used in HPLC was LUNA 5${\mu}$ C18 (250 ${\times}$4.6mm) (Phenmenex Co.m Torroance, CA, U.S.A.). (omitted)

• Advances in nano research
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• 제13권3호
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• pp.217-231
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• 2022

This study investigates the geometrical impact on the nanomedicine drug delivery via nanodevices. A nanomotor made of the nanotube carrying the drug as the motor blade is considered in the blood flow. Physical activities change the blood flow, and sports training enhances the blood flow and plays a significant role in the stability of drug delivery devices. This paper studies the impact of geometrical parameters on the nanomotors carrying the nanomedicine. The effect of physical exercise on the dynamic response regarding the stability of drug delivery devices is discussed in detail.

• Bulletin of the Korean Chemical Society
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• 제32권6호
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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 Pharmaceutical Investigation
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• 제41권4호
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• pp.227-232
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• 2011

Alnus japonica has been known to exert antioxidative, anti-inflammatory, anti-cancer and immune response inhibitory effects. The aim of this study was to figure out the characteristics of extracts obtained with different extraction solvent such as water, 100% ethanol, 70% ethanol or 70% methanol because characteristic components such as oregonin and hirsutanone extracted from Alnus japonica might be essential for the biological activity. For this purpose, oregonin and hirsutanon of four extracts, index ingredient of Alnus japonica, were analyzed with HPLC and physicochemical studies such as SEM, particle size and zeta potential were conducted. In cell cytotoxicity study, extract of water showed the highest cytotoxicity among four extracts. In case of oregonin, 70% MeOH and water extracts showed high contents and in case of hirsutanone, all extracts showed similar contents except 70% EtOH extracts. The extract of 70% MeOH from Alnus japonica for both oregonin and hirsutanone appeared to have the highest content. Both oregonin and hirsutanone extracted from Alnus japonica using 70% methanol showed stability in pH 1.2.

• Toxicological Research
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• 제29권1호
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• pp.1-6
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• 2013

The process of drug discovery and development requires substantial resources and time. The drug industry has tried to reduce costs by conducting appropriate animal studies together with molecular biological and genetic analyses. Basic science research has been limited to in vitro studies of cellular processes and ex vivo tissue examination using suitable animal models of disease. However, in the past two decades new technologies have been developed that permit the imaging of live animals using radiotracer emission, X-rays, magnetic resonance signals, fluorescence, and bioluminescence. The main objective of this review is to provide an overview of small animal molecular imaging, with a focus on nuclear imaging (single photon emission computed tomography and positron emission tomography). These technologies permit visualization of toxicodynamics as well as toxicity to specific organs by directly monitoring drug accumulation and assessing physiological and/or molecular alterations. Nuclear imaging technology has great potential for improving the efficiency of the drug development process.

• 약학회지
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• 제52권5호
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• pp.331-344
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• 2008

Recently, the FDA (Food and Drug Administration) of the United States and many advanced countries remark biomarkers and surrogate endpoints as a critical path tool on model based drug development. Economic, technical and social profit on model based drug development like a reduction of the length of research and development have been achieved. Therefore we summarize previous studies about biomarkers and surrogate endpoints and suggest a development direction of therapeutic agents. In diabetes mellitus (DM) and osteoporosis, there are remarkable increases in number of patients and most of patients take medicine during their whole lifetime. For this reason, many patients with DM and osteoporosis have a tolerance on their medicine. We expect that research and development on biomarkers and surrogate endpoints will contribute to new drug development on DM and osteoporosis. Biomarkers for DM are blood levels of glucose, insulin, ${HbA}_{1c}$, CRP, alpha-glucosidase, adiponectin and DPP-4. Among these, validated surrogate endpoints for DM are blood levels of glucose, insulin and ${HbA}_{1c}$ Biomarkers for osteoporosis are BMD, BMC, trabecular volume, ICTP, DPD, osteocalcin, the activity of osteoclast and production of osteoblast. The validated surrogate endpoints for osteoporosis are BMD only. This review summarizes all suggested biomarkers and surrogate endpoints in DM and osteoporosis. The biomarkers are classified by drugs, and the method of validation for surrogate endpoints is suggested. This information would contribute to suggest a direction of DM and osteoporosis therapeutic agent development.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.240.2-241
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• 2001