• Bulletin of the Korean Chemical Society
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• v.35 no.1
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• pp.129-134
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• 2014

Two series of SAHA-liked hydroxamate analogues were designed, synthesized and evaluated for their biological activities against nuclear HDACs. Compounds of Series I were found to be very effective inhibitors of cancer cell growth in the PC-3, Hut78, K562 and Jurkat E6-1 cancer cell lines with mean $IC_{50}$ values from $0.54{\mu}M$ (Ic, Jurkat E6-1) to $7.73{\mu}M$ (Ib, K562), indicating that they are cell permeable and the benzimidazolyl-based ligands are flexible enough to occupy the binding site of HDAC.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.420-423
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• 1994

Various N'-substituted anilino-N-methyl-N'-nitrosoureas(2a-n) were easily prepared from the reaction of substituted phenylhydraines $(3, 4-CH_3, {\;} 3-, {\;} 4-OCH_3, {\;} 3-, {\;} 4-F, {\;} 3, {\;} 4-Cl, {\;} 4-Br, {\;} 2-, {\;} 3-, {\;} 4-NO_2, 4-(NO_2)_2)$ with methyl isocyanate, followed by the nitrosation with 99% HCOOH and dry sodium lnitrite powder. Surprisingly, of these series of analogus, the anilino-nitrocosureas substituted with eletron-withdrawing nitro groups (2k-a) showed significantly low $ED_{30}$ values of $1.4-3.4 {\mu}g/ml.$ In addition, none of these copounds subtituted with electron-donating groups exhibited cytotoxicities.

• IMMUNE NETWORK
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• v.20 no.1
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• pp.3.1-3.20
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• 2020

Immune checkpoint inhibitors (ICIs), including anti-PD-1 and anti-CTLA-4 therapeutic agents, are now approved by the Food and Drug Administration for treatment of various types of cancer. However, the therapeutic efficacy of ICIs varies among patients and cancer types. Moreover, most patients do not develop durable antitumor responses after ICI therapy due to an ephemeral reversal of T-cell dysfunction. As co-stimulatory receptors play key roles in regulating the effector functions of T cells, activating co-stimulatory pathways may improve checkpoint inhibition efficacy, and lead to durable antitumor responses. Here, we review recent advances in our understating of co-stimulatory receptors in cancers, providing the necessary groundwork for the rational design of cancer immunotherapy.

• Korean Journal of Pharmacognosy
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• v.30 no.2
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• pp.130-136
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• 1999

The cytotoxic and antitumor activity of Herba cratalariae sessiliflorae on cultured NIH 3T3 fibroblast and human oral epitheloid carcinoma cells were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) colorimetric method. The light microscopic study was carried out to observe morphological changes of cultured mouse fibroblast and human oral epitheloid carcinoma cells (KB). These results were obtained as follows; Ethyl acetate, chloroform and hexane extracts showed a significant cytotoxicity in NIH 3T3 fibroblast, but the other extracts did not show. All extracts exhibited a significant antitumor activity in human oral epitheloid carcinoma cells, but ethanol extract did not show a antitumor activity. Hexane extract showed low cytotoxic effect, but exhibited the most antitumor activity. The MTT absorbance in NIH 3T3 fibroblast was significantly decreased by treatment with chloroform, ethyl acetate and hexane extracts respectively. Human oral epitheloid carcinoma cells was significantly decreasd by treatment with all extracts with the exception of ethanol extract. The difference in MTT absorbance in two cell Types was most remarkable when treated with water and hexane extracts. Cholroform and hexane extracts showed the strongest effect in growth inhibition of human oral epitheloid carcinoma cells. These results indicated that water extract possessed no cytotoxicity and a strong antitumor activity.

• The Korean Journal of Food And Nutrition
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• v.27 no.5
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• pp.837-844
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• 2014

This study was carried out to analyze the differences in p-hydroxylbenzyl alcohol (HBA) content, antitumor and anti-obesity activities and tyrosinase inhibitory activity between non-fermented G. elata (NFGP) and fermented G. elata powder. The HBA content, which is an index-component of G. elata decreased from 1.58 mg/g before fermentation to 1.07, 0.32, and 0.13 mg/g after the $1^{st}$ fermentation ($1^{st}$ FGP), $2^{nd}$ fermentation ($2^{nd}$ FGP) and $3^{rd}$ fermentation ($3^{rd}$ FGP), respectively. The anti-proliferation effects on the cell lines HT29 and AGS were significantly higher for the fermented G. elata than the NFGP. The antitumor activity was also increased in a fermentation number-dependent manner. During adipocyte differentiation, the ethanol extract of the $3^{rd}$ FGP inhibited lipid accumulation in 3T3-L1 cells significantly better than NFGP and the $1^{st}$ FGP, treated at the concentration of $10{\mu}g/mL$. The tyrosinase inhibitory activity of the $2^{nd}$ FGP at $600{\mu}g/mL$ over was higher than that of kojic acid. At the concentration of $1,000{\mu}g/mL$, the tyrosinase inhibitory activity was increased in a fermentation number-dependent manner. From these results, the fermented G. elata, especially the $3^{rd}$ FGP, is expected to be good candidate for the development of functional food and agents with antitumor, anti-obesity, and tyrosinase inhibitory potential.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.3
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• pp.915-921
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• 2015

Context: In the last half century, discovering, developing and introducing of clinical agents from marine sources have seen great successes, with examples including the anti-cancer compound trabectedin. However, with increasing need for new anticancer drugs, further exploration for novel compounds from marine organism sources is strongly justified. Objective: The major aim of this study was to evaluate the antitumor and antioxidant potential of Sargassum tenerrimum J.Agardh (Sargassaceae) on Ehrlich ascites carcinoma (EAC) in Swiss albino mice. Materials and Methods: An ethanol extract of S. tenerrimum (EEST) from whole algae was used to evaluate cytotoxicity followed by in vivo assessment of toxicity, using biochemical parameters including hepatic and non-hepatic enzymes. Antioxidant properties were examined in animals bearing EAC treated with daily oral administration of 100-300 mg/kg extract suspension. Results: Antitumor effects of EEST in EAC bearing mice was observed with LD50 1815 mg/kg. Parameters like body weight, tumor volume, packed cell volume, tumor cell count, mean survival time and increase in life span in animals in the EAC bearing animals treated with EEST 300 mg/kg was comparable with control group. Significant differences were also seen with changes in total protein content, hepatic enzymes contents, MDA level, and free radical scavenging enzymes in untreated vs. EEST treated group animals. Conclusions: Evaluation of antioxidant enzymes and hepatic enzymes in the EAC animal model treated with EEST exhibited similar effects as the positive control drug 5-flurouracil. S. tenerrimum extracts contain effective antioxidants with significant antitumor activity.

• Archives of Pharmacal Research
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• v.11 no.3
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• pp.169-174
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• 1988

A new series of substituted phenazone derivatives has been prepared through a series of reactions that are illustrated in Scheme I. The antibacterial and antineoplastic activities of the prepared compounds were evaluated. While none of the synthesized products showed marked antibacterial activity, all of them possessed a significant antitumor effect.

• Korean Journal of Pharmacognosy
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• v.23 no.4
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• pp.264-267
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• 1992

The cytotoxic activity of medicinal plants was screened using A549 human lung cancer cell line. Plant materials were extracted with 80% methanol and fractionated to chloroform and water layers. Each methanol, chloroform, and water extract of thirty-two medicinal plants was tested for cytotoxic activity in A549 cell culture system and the cell viability was measured by SRB assay.

• Archives of Pharmacal Research
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• v.24 no.5
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• pp.385-389
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• 2001

Twelve 4-substituted cyclopenta[c]quinoline derivatives were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, MD-MB-468 and T-47D). The compounds 6c and 6e bearing p-anisidine and pyrrolidine side chain were more active than the others.

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.234.3-235
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• 2001