• Archives of Pharmacal Research
• /
• v.20 no.3
• /
• pp.264-268
• /
• 1997

In order to study the structure-activity relationship of 7, 8-dimethoxy-2-methyl-3-(4, 5-methylenedioxy-2-vinylphenyl)isoquinoline-1(2H) -one (2), which has exhibited significant antitumor activity, chemical modifications of 2 were performed to yield the corresponding products (3-7). Further systematic uses of an efficient procedure for the synthesis of 3-arylisoquinoline derivatives produced the substituted compounds (9a-9g), which were tested for in vitro antitumor activity against five different human cancer cell lines.

• Archives of Pharmacal Research
• /
• v.26 no.6
• /
• pp.441-445
• /
• 2003

New sulfonated amino ribofuranans were synthesized to elucidate the relationship between structure and specific biological activities such as anti-HIV and blood anticoagulant activities. The synthesis was performed by sulfonation of copolymers having various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranosidic unit. The sulfonation with piperidine N-sulfonic acid produced the sulfonated amino ribofuranans in high yield. The anti-HIV activity of sulfonated 3-amino-3-deoxy-(1$\rightarrow5)-\alpha$-D-ribofuranan showed more potent by increasing the degree of sulfonation and the average molecular weights. This activity was almost equal to the activities of sulfonated ribofuranans and ribopyranans reported before in spite of low molecular weight. The blood anticoagulant activities was observed at 36-48 mg/units, more potent than standard dextran sulfonate, 22.7 mg/units. In addition, the blood anticoagulant activities of sulfamide-copolysaccharide consisting various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranan units were potentiated by increasing sulfonated amino-ribofuranan units from 13 to 21 mg/units.

• Proceedings of the Korean Vacuum Society Conference
• /
• 2010.02a
• /
• pp.34-34
• /
• 2010

Activities of various $TiO_2$ nanostructures in photocatalytic decomposition of methylene blue and toluene were determined in order to shed light on the relationship between structures and photocatalytic activity. Commercially available P-25 samples were used in the present work. In addition, $TiO_2$ nanostructures were synthesized using atomic layer deposition (ALD). We show that change in the surface structure of $TiO_2$ upon variois surface treatments results in variation in photocatalytic activity. In particular, increase in the number of OH groups on the surface leads to the enhancement in photocatalytc activity. Surface OH groups increases adsorption reactivity of organic reactants, thereby increasing activity in photocatalytic decomposition of methylene blue and toluene.

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.372.1-372.1
• /
• 2002

AIzelin (1) and quercitrin (2) isolated from the EtOAc-soluble fraction of the leaves of Litsea japonica Jussieu (Lauraceae) showed inhibitory activity against classical pathway complement system with 50% inhibitory concentration ($IC_{50}$/) values of 112.2 and 198.2 $\mu\textrm{g}$/$m\ell$. respectively. For the structure-activity relationship of flavonoids on anti-complement system. myricitrin (3) from JUQ/ans mandshurica Maximowicz (Juglandaceae) also tested anti-complement activity. while this was devoid of any significant activity. (omitted)

• Archives of Pharmacal Research
• /
• v.21 no.2
• /
• pp.207-211
• /
• 1998

Three prolyl endopeptidase inhibitors were isolated and identified as luteolin, quercetin and ${\beta}$-sitosterol-3-O-${\beta}$-D-glucopyranoside with $IC_{50}$ of 0.17, 0.19 and 27.5 ppm, respectively. The inhibition of two flavonoids were non-competitive with substrate. Twenty authentic flavonoids were tested in order to investigate structure-activity relationship. No significant relationship was found in them, however, catechol moiety of B-ring and 7-OH group in flavonoid skeleton were seemed to be responsible for the stronger activity.

• Proceedings of the Korean Society of Toxicology Conference
• /
• 2003.10b
• /
• pp.64-67
• /
• 2003

Halogenated aromatic hydrocarbons (HAHs) including TCDD and PCBs are known to cause neurotoxic effects in both man and animals such as cognitive impairment and motor dysfunctions. While theses chemicals may lead to neurodevelopmental and neurobehavioral deficit, structural activity relationship and molecular targets for these chemicals are not elucidated.(omitted)

• Bulletin of the Korean Chemical Society
• /
• v.29 no.6
• /
• pp.1125-1130
• /
• 2008

A series of dihydroxylated chalcone derivatives with diverse substitution patterns on a phenyl ring B and the para-substituents on a phenyl ring A were prepared, and their radical scavenging activities were evaluated by simple DPPH test to determine quantitative structure-activity relationship in these series of compounds. The chalcone compounds with the ortho- (i.e. 2',3'- and 3',4'-) and para- (i.e. 2,5'-) substitution patterns show an excellent antioxidant activities (80-90% of control at the concentration of 50 $\mu$M) which are comparable to those of ascorbic acid and $\alpha$ -tocopherol as positive reference materials. On the contrary, the compounds with meta- (i.e. 2',4'-, 3',5'-) substitution pattern demonstrate very dramatic decrease in activities which are around 25% of the control even at the concentration of 200 $\mu$ M (IC50 > 200 $\mu$ M). These dramatic differences could be interpreted in terms of the ease formation of fairly stable semiquinone radicals from the ortho- and parasubstituted chalcone molecules through facilitating electron delocalization. Our results indicate that the substitution patterns of two hydroxyl groups on ring B are very important structural factors for their radical scavenging activity enhancement. Meanwhile, the substituents at para-position of the phenyl ring A of chalcones have no influence on the activity.

• Journal of Digital Convergence
• /
• v.17 no.1
• /
• pp.443-447
• /
• 2019

Aryl hydrocarbon receptor (AhR) is the master regulator of xenobiotics metabolizing enzymes (XMEs). AhR is activated by aryl hydrocarbons upon binding then goes into the cell nucleus and acts as a transcription factor. Despite the role of AhR in human physiology has been investigated for a long while, it is yet to be understood mainly due to the lack of appropriate chemical agents. Furthermore, it has been reported that AhR is related to a wide range of pathogenesis. In addition, recent studies suggest that the study on the development of AhR antagonist may provide a valid therapeutic agent. Some known antagonists in current use are partially agonistic whereas a pure antagonist is still absent. In this study, two phenyl-ring structures of phenyldiazenylphenylpicolinamide has been modified into various structures and evaluated its impact on the AhR antagonistic activity to elucidate the structure-activity relationship.

• Industrial Engineering and Management Systems
• /
• v.15 no.3
• /
• pp.251-258
• /
• 2016

Companies have developed a keen interest in bolstering their CSR activities. Especially in Japan, CSR is strongly associated with social contribution and $m{\acute{e}}c{\acute{e}}nat$ activities. On the other hand, the primary purpose of companies is to provide their products and services to consumers and thereby return value to their shareholders through sales and profits. It is, however, difficult to estimate directly the relationship between CSR and sales/profits. This study focuses particularly on CSR activities related to environmental and consumer issues and community involvement and development. It is also analyzed the relationship between the degree of CSR empathy and product purchase motivation. For accomplishment the purpose, a questionnaire is designed that elicits the respondent's degree of purchase intention and empathy toward CSR activities supported through sales. The object industry for questionnaires is TV maker. For results of the questionnaire, a covariance structure analysis is conducted to understand potential relationships among CSR activities, sales, and disposable budget. Through this study, it is able to clear the relationship between CSR activities and sales/profits. It is one of the advice to future prospect, strategy and CSR concept for the companies.

• Journal of Aquaculture
• /
• v.19 no.1
• /
• pp.33-39
• /
• 2006

Anticoagulant activities of a fermented edible brown alga, Laminaria ochotensis was investigated. L. ochotensis was fermented with 15% sugar (w/v) at $25^{\circ}C$ for 10 weeks. Anticoagulant activity was measured from the supernatant of algal mixture at biweekly intervals up to $10^{th}$ week by activated partial thromboplastin (APTT), prothrombin time (PT) and thrombin time (TT) assay using citrated human plasma. Sample having high APTT activity $(6^{th}\;week)$ was filtered, ethanol precipitated and freeze-dried. The polysaccharide compound having anticoagulant activity was purified by DEAE ion exchange chromatography followed by Sepharose-4B gel filtration chromatography. Anticoagulant activity, polysaccharide concentration, and heparin like activity were determined for the collected fractions by APTT, $phenol-H_2SO_4$, and glycosaminoglycan assay, respectively. The anticoagulant activity assay showed that the activity was increased up to $6^{th}$ week, and decreased thereafter. The concentration of our purified compound was $31.0{\mu}g/ml$ and showed higher APTT activity than commercial heparin. At the same concentration of $31.0{\mu}g/ml$, the heparin showed 186.5 sec activity while our purified compound showed an activity of 386 sec. Single spot on agarose gel electrophoresis showed that the compound was purified and polyacrylamide gel electrophoresis (PAGE) results revealed that the molecular mass of the purified polysaccharide compound was between 60 and 500 kDa. Therapeutic interest of the algal polysaccharide as an anticoagulant has recently been in highlighted. This purified anticoagulant compound from fermented L. ochotensis can be used as a model for anticoagulant agent or could be developed as an anticoagulant agent. This study can be extended to identify the structure and chemical composition of the purified polysaccharide, and to establish a relationship between structure and the function of the identified anticoagulant compounds.