• Proceedings of the PSK Conference
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• 2002.10a
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• pp.348.2-348.2
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• 2002

The significant antitumor activities of 3-arylisoquinolines promoted us to explore the structure-activity relationship of these compounds. A series of 3-Arylisoquinoline derivatives, which related to Benzo［c］ phenanthridine alkaloids. were evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). We tried to study structure-activity relationship (SAR) of 3-Arylisoquinolines using the comparative molecular field analysis (CoMFA) method. (omitted)

• YAKHAK HOEJI
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• v.55 no.2
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• pp.154-159
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• 2011

During the search for a novel compound that can inhibit NF-${\kappa}B$ activation, 6-hydroxy-7-methoxychroman-2-carboxylic acid phenyl amide (KL-1156) was identified as a good inhibitor of NF-${\kappa}B$ activation. In the present study, we describe the synthesis of methylchroman-2-carboxylic acid N-(disubstituted)phenylamide derivatives (1 and 2 serieses). In addition, their inhibitory effects of NF-${\kappa}B$ are compared with activity of KL-1156 and SAR (structure activity relationship) are explored.

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.556-562
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• 2006

Ten semi-synthetic derivatives of asiatic acid were prepared and their wound healing effects were evaluated by employing a tensile strength assay and a wound area assay. Among them, ethoxymethyl 2-oxo-3,23-isopropylidene-asiatate (12) showed the strongest and the fastest wound healing activity. Furthermore, it left the smallest scar after healing.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.340.1-340.1
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• 2002

Centella asiatica is an herbal plant used on different continents by diverse ancient cultures and tribal groups. Historically. the extract has been used as a wound healing agent, The extract has three different triterpenoid ingredients: asiaticoside. asiatic acid, and madecassic acid. It has been reported that its wound healing activity is associated with the modulation of collagen synthesis in the skin dermis. The wound healing property of the extract has led to its commercial introduction under the trade name, Madecrlssol. As part of our program toward the development of new wound healing agents. structere activity relationship (SAR) studies have been performed by modifying asiatic acid. In this communication. the SAR study of esiatic acid for the development of an efficient woind healing agent is reported.

• Bulletin of the Korean Chemical Society
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• v.31 no.8
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• pp.2315-2321
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• 2010

Twenty spirodiclofen analogues have been designed and conveniently synthesized via three steps including esterification, one-pot heterocyclization, and acylation reactions. The target molecules have been identified on the basis of analytical spectra ($^1H$ NMR, $^{13}C$ NMR and ESI-MS) data. All newly synthesized compounds have been screened for their potential insecticidal and herbicidal activity by standard method. The preliminary assays indicated that some of analogues displayed moderate to good insecticidal activity against Plutella xylostella compared with spirodiclofen, and some compounds showed obvious activity against Brassica chinensis. Structure-activity relationship (SAR) is also discussed based on the experimental data.

• 한국지구물리탐사학회:학술대회논문집
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• 2003.11a
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• pp.305-312
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• 2003

Remote sensing can provide invisible information in addition to acquire wide-view image data from space. Synthetic Aperture Radar (SAR) transmits microwave to the earth from a satellite and collects the reflected echo from the surface. Interferometric processing of SAR data can detect the subtle land deformation. The information of the surface movement by SAR is useful to monitor the volcanic activity, extended subsidence of urbanized area and the prediction of the earthquake caused by crustal deformation, and it complements the conventional levelling and GPS technique. PSInSAR (Permanent Scatterers Interferometric SAR) is one of interferometric techniques to be applied to practical projects in Japan. In this paper, the projects of land deformation monitoring are shown after the explanations of the PSInSAR principle. Tokai earthquake risk assessment is the first example. PSInSAR detects the subduction of crustal deformation of the adjacent area of new assumed epicenter region of the Tokai Earthquake. The extended subsidence of the urbanized area was implemented by using Japanese satellite data i.e. JERS that has so much data the surrounding of Japan as the archive. We examine the relationship between the geological structure and settlement at Nohbi basin including Nagoya city.

• Bulletin of the Korean Chemical Society
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• v.22 no.10
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• pp.1067-1068
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• 2001

• Bulletin of the Korean Chemical Society
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• v.32 no.10
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• pp.3566-3570
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• 2011

A series of 2,4,6-tripyridyl pyridines were synthesized, and evaluated for their antitumor cytotoxicity, topoisomerase I and II inhibitory activity. From the eighteen prepared compounds, compounds 10-12 have shown better or similar cytotoxicity against several human cancer cell lines as compared to 2,2':6',2"-terpyridine and doxorubicin. Especially, compound 10 exhibited the most potent cytotoxicity better than positive controls. Structure-activity relationship study indicated that 2,2':6',2"-terpyridine skeleton has an important role in displaying significant cytotoxicity against several human cancer cell lines.

• Applied Biological Chemistry
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• v.42 no.3
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• pp.252-255
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• 1999

Inhibition activities$(pI_{50})$ of chalcone derivatives as substrate with farnesyl protein transferase(FPTase) were determined in vitro. The structure activity relationships(SAR) between the activity and physicochemical parameters of X & Y-substituents on the phenyl groups were analyzed by Free-Wilson and Hansch method. X-substituents on the benzoyl group have the more important role to inhibition activity than Y-substituents on the styryl group. Among them, none substituent, 8 showed the highest FPTase inhibition activity$(pI_{50}=4.30)$. Particularly, the SAR equation could be formulated, showing a parabolic relationship between the activity and hydrophobicity(logP) where the optimal value$({\Sigma}logP)_{opt}$ was 3.915. And also the activity depends on the steric effect(Es > 0) with X-substituent and the resonance effect(R < 0) with electron donating Y-substituents. Based on the results of SAR analyses, the interactions between substrates and receptor, FPTase, could be assumed.

• Biomolecules & Therapeutics
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• v.31 no.2
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• pp.176-182
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• 2023

Among 14 subtypes of serotonin receptors (5-HTRs), 5-HT_2AR plays important roles in drug addiction and various psychiatric disorders. Agonists for 5-HT_2AR have been classified into three structural groups: phenethylamines, tryptamines, and ergolines. In this study, the structure-activity relationship (SAR) of phenethylamine and tryptamine derivatives for binding 5-HT_2AR was determined. In addition, functional and regulatory evaluation of selected compounds was conducted for extracellular signal-regulated kinases (ERKs) and receptor endocytosis. SAR studies showed that phenethylamines possessed higher affinity to 5-HT_2AR than tryptamines. In phenethylamines, two phenyl groups were attached to the carbon and nitrogen (R³ ) atoms of ethylamine, the backbone of phenethylamines. Alkyl or halogen groups on the phenyl ring attached to the β carbon exerted positive effects on the binding affinity when they were at para positions. Oxygen-containing groups attached to R³ exerted mixed influences depending on the position of their attachment. In tryptamine derivatives, tryptamine group was attached to the β carbon of ethylamine, and ally groups were attached to the nitrogen atom. Oxygen-containing substituents on large ring and alkyl substituents on the small ring of tryptamine groups exerted positive and negative influence on the affinity for 5-HT_2AR, respectively. Ally groups attached to the nitrogen atom of ethylamine exerted negative influences. Functional and regulatory activities of the tested compounds correlated with their affinity for 5-HT_2AR, suggesting their agonistic nature. In conclusion, this study provides information for designing novel ligands for 5-HT_2AR, which can be used to control psychiatric disorders and drug abuse.