• Bulletin of the Korean Chemical Society
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• 제26권12호
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• pp.2047-2050
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• 2005

• 생명과학회지
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• 제8권1호
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• pp.67-71
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• 1998

다량의 시료를 빠르게, 적은 격비로, 간다히 검색할수 있는 예비선별법을 찾던중, ccDNA와 sulforhodamine B를 각각 사용한 미생물배양액내의 신규항암후보물질의 탐색을 시도하였다. cccDNA법으로는 3.3%가 positive 반응을 나태내었으며, SRB assat에서는 A549와 SK-OV-3에 활성을 나타내는 4개의 발효여액을 확인한수 있었다.

• 동의생리병리학회지
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• 제19권2호
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• pp.441-445
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• 2005

Tripterygium regelii has been used as an oriental medicine, especially antiparasitic, anti-inflammatory and detoxifying agents in East asia. During our research to develop new antitumor agents from natural products, MeOH ext. and CH2Cl2 ext. of Tripterygium regelii showed the potent antitumor activity. In order to purify active compounds from Tripterygium regelii, activity-guided fractionation was carried out. Silica gel and RP-18 column chromatography for the active fraction led to the isolation of two compounds and their antitumor activities were studied. Those two compounds didn't show potent antitumor activity against human tumor cell lines. The structure of two compounds were determined by $^1H-NMR$, $^{13}C-NMR$, DEPT, $^1H-^{13}C$ COSY and IR spectrum. Compound I and Compound II were turned out to be Celastrol, and ${\beta}-sitosteryl-3-o-{\beta}-D-glucopyranoside$ respectively.

• Bulletin of the Korean Chemical Society
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• 제31권6호
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• pp.1463-1464
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• 2010

• Archives of Pharmacal Research
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• 제25권4호
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• pp.416-420
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• 2002

A series of isoindoloquinoline derivatives was synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HCT15, SK-OV-3, MDA-MB-468 and T-47D).

• Biomolecules & Therapeutics
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• 제9권3호
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• pp.143-155
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• 2001

Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.610-619
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• 1997

Some new 9H-thioxanthen-9-one incorporated into heterocyclic systems such as pyridone 8, pyrazoline 9, pyranone 11, iminopyrane 12, furopyrimidine 17, imidazothiazole 19, thiazole 21, triazine 24 and other related compounds through a para imminophenyl grouping at position-1 of the thioxanthenone ring were synthesized and tested as antitumor agents against L1210 leukemia in mice. Some of the new compounds showed considerable antitumor activity.

• 약학회지
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• 제26권3호
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• pp.181-184
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• 1982

The iron and copper chelates of 4-dimethylamino-2-formylpyridine thiosemicarbazone, one of the amine substituted derivatives at 4-C of 2-formylpyridine thiosemicarbazones which are known as the more improved potential antitumor agents, have been synthesized to make them more effective than the ligand (denoted as HL) itself. Their ligand-to-metal ratios were 2:1 and 1:1 for the iron and copper chelates, and the data along with those of elemental analysis and IR spectroscopy showed that. the compositions are [$FeI_{2}{\times}2H_{2}SO_{4}$ and [CuL($H_{2}Cl$O)], respectively.

• 생약학회지
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• 제29권1호
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• pp.22-27
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• 1998

This study was carried out to develop antitumor agents based on effects of the ethyl acetate soluble fraction of the methanolic extract of Lonicerae flos on human oral epitheloid carcinoma cells. Human oral epitheloid carcinoma cells were cultured in RPMI-1640 media containing 10% fetal bovine serum, antibiotic, and fungizone. After incubation for 24 hrs, the cells were treated with A, B, C, D, and E fractions for 48hrs under the same condition. MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide), NR (Neutral red) and SRB (Sulforhodamine B protein) assay were performed. The light microscopic findings were observed by inverted microscope. In MTT assay, fraction B was shown significant antitumor activity (P<0.001), fraction E was shown significant antitumor activities (P<0.05), but the other fractions were not shown. In NR assay, fraction B was shown significant antitumor activity (P<0.001). In SRB assay, fractions B was shown significant antitumor activities (P<0.01). fractions A and D were shown significant antitumor activities (P<0.05). but the other fractions were not shown. In light microscopy. the fraction B of the ethyl acetate soluble fraction of the methanolic extract of Lonicerae flos showed the highest antitumor activity. These finding suggested that fraction B possessed the most antitumorous agent.

• 분석과학
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• 제23권6호
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• pp.579-586
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• 2010

현재 상업적으로 널리 사용 되여 지고 있는 항암제인 hydroxy urea, 6-mercaptopurine monohydrate, cytosine arabinoside, cyclophosphamide monohydrate 그리고 uracil를 3-(triethoxysilyl) propyl isocyanate 와 반응시켜 항암제가 붙어있는 3-(triethoxysilyl)propyl amide (compound I)을 합성한후 물과 가수분해 반응시켜 항암제가 결합된 silica 나노입자(10 nm~micronparticles)를 만들 수있었다. Silyl isocyanate 유도체들은 물과 반응하여 유기물질-silica 나노입자가 포함된 $-CH_2-CH_2-CH_2-NH-COOH$ 그룹이나 혹은 온도와 용매등 반응조건에 따라서 decarboxylated 된 propylamine 그룹이 생성되었다. 생체외 시험에서 항암제가 결합된 silica 나노입자는 종양 세포 제거에 효과적이고 정상세포에 거의 영향을 미치지 않는 것으로 나타났다. 그리고 악성 종양인 폐, 난소, 악성 흑색종, 중추신경계(CNS)와 결장 종양 세포가 이 연구에 사용되었다. 현재의 연구에서 전달매체 로서 silica는 silation 반응으로 손쉽게 나노입자를 얻을 수 있으므로 본 연구에 쉽게 이용 할 수 있다. 결과로부터 이 기술은 보다 부작용이 적은 생체 의약품에 적합한 carrier nanoparticles에 적용 될 수 있을 것으로 판단된다.