• 통합자연과학논문집
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• 제7권3호
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• pp.159-165
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• 2014

Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• 대한화학회지
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• 제56권2호
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• pp.251-256
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• 2012

A novel series of benzothiazole derivatives were synthesized and assayed in vivo to investigate their hypoglycemic activity by streptozotocin-induced diebetic model in rat. These derivatives showed considerable biological efficacy when compared to glibenclamide, a potent and well known antidiabetic agent as a reference drug. All the compounds were effective, amongst them 3d showed more prominent activity at 100 mg/kg p.o. The experimental results are statistically significant at p<0.01 and p<0.05 level.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.101-101
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• 1997

As part of a drug discovery program to develope more effective platinum-based anticancer drugs, a series of platinum complexes trans -diaminocyclohexane platinum bi sdiphenylphosphino -ethane (KHPC-002) cis-diaminocyclohexane platinum bisdiphenylphosphino-ethane (KHPC-006) has been evaluated in vitro against 4 human carcinoma cell lines with those of cisplatin using a tetrazolium-based colorimetric assay (MTT assay). The cell lines were two human bladder carcinoma cell lines, HT-1197 and HT-1376, human colon carcinoma cell line, HCT-116, and prostate cancer cell line DU-145.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.111-111
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• 1997

As part of a drug discovery program to develope more effective platinum-based anticancer drugs, a series of platinum complexes trans-diaminocyclohexane platinum bi sdiphenylphosphino - ethane ( KHPC- 002) cis-diaminocyclohexane platinum bi sdiphenylphosphino - ethane ( KHPC- 006) has been evaluated in vitro against 4 human carcinoma cell lines with those of cisplatin using a tetrazolium-based colorimetric assay (MTT assay). The cell lines were two human bladder carcinoma cell lines, HT-1197 and HT-1376, human colon carcinoma cell line, HCT-116, and prostate cancer cell line DU-145. in vitro cytotoxic potential of each platinum complex was expressed as the cytotoxicity index (Cl, %).

• 통합자연과학논문집
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• 제8권3호
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• pp.204-208
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• 2015

Pyrazole, ${\beta}$-lactam, salicidine, pyren and oxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against COX-2 enzyme. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Natural Product Sciences
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• 제26권2호
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• pp.109-117
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• 2020

The canonical Wnt/β-catenin signaling pathways play an important role in the embryonic development, cell proliferation, differentiation, and adhesion. Therefore, the abnormal activation and repression have been associated with uncontrolled homeostasis in human tissues. In particular, the activation of Wnt signaling is highly correlated with a diverse of diseases including cancer. On this regard, a strategy for targeting Wnt/β-catenin signaling has been employed in the discovery and development of antitumor agents. Herein, the evolution of Wnt signaling and the Wnt inhibitors derived from natural products were briefly summarized in the drug discovery of anticancer agents.

• Biomaterials and Biomechanics in Bioengineering
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• 제1권2호
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• pp.73-79
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• 2014

Covalent attachment of 1, 4-dimethylnaphthalene (DMN) based endoperoxide forming subunits to a polyvinyl butyral (PVB) backbone has been achieved. The functionalized polymer materials prepared and characterized here can serve as biocompatible carrier systems for studying cellular uptake, intermediate storage and delayed release of singlet oxygen, which opens up new doors for optimizing a variety of medical applications of photogenerated DMN-endoperoxides such as antiviral, antibacterial, antiplasmodial and antitumor activity.

• Applied Biological Chemistry
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• 제34권2호
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• pp.86-93
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• 1991

CDDP는 $100\;{\mu}M$ 이하의 농도에서 BTV 캡시드 단백질에 crosslink를 형성하지 않는다. 밀도구배초원심분리 결과에 의하면 캡시드 단백질과 RNA사이의 crosslink도 일어나지 않는다. CDDP를 처리한 BTV RNA를 폴리아크릴아마이드 겔에 전기연동하면 RNA이동 패턴이 변한다. 이 결과는 BTV core에 없는 RNA중합효소의 불활성화가 CDDP에 의한 BNA RNA의 구조변화에 의함을 가리킨다.

• Archives of Pharmacal Research
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• 제20권2호
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• pp.176-179
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• 1997

Purine nucleosides were chlorinated by the reaction of acyl chloride in DMF with MCPBA under mild conditions with moderate yields. And, satisfactory method for the synthesis of ribonucleoside-$3^{I},5^{I}$-cyclic phosphates and its characterization by$^{1}H$ and $^{13}C$ nmr spectroscopy is described.

• 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.180.1-180.1
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• 2003

Eukaryotic DNA topoisomerase I (top I) is an essential enzyme that act to relax supercoiled DNA during the transcription, replication and mitosis. Intracellular levels of top I are elevated in a number of human solid tumors, relative to the respective normal tissues, suggesting that controlling the topI level is important to treat cancer. Top I poisons show their antitumor activities by stabilizing the cleavable ternary complex consisting of top I enzyme, DNA, and drug. Thus, top I is a promising target for the development of new cancer chemotherapeutics against a number of solid tumors. (omitted)