• Archives of Pharmacal Research
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• 제29권10호
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• pp.826-833
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• 2006

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

• Preventive Nutrition and Food Science
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• 제5권1호
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• pp.54-57
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• 2000

This study was designed to observe the anticancer activity of propolis on human rectal (HRT-18) and human colon (HCT-48) cancer cell lines in vitro, and on sarcoma-180 cells in vitro. The proliferation of HRT-18 and HCT-48 cancer cell lines was potently inhibited in proportion to the concentration of propolis. The survival time of the mice inoculated with sarcoma-180 cells was increased modestly by the administration of propolis compared to the control. Those observations suggest that propolis has anticancer effects against some of the cancer cell lines in vitro and in in vitro.

• Bulletin of the Korean Chemical Society
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• 제30권1호
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• pp.83-91
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• 2009

To develop new anticancer agents, 3-allylthio-6-aminopyridazine derivatives were synthesized from maleic anhydrides or phthalic anhydrides by formation of a pyridazine nucleus, dichlorination, allylthiolation and amination. The pyridazine nuclei were obtained by condensing a hydrazine monohydrate with maleic anhydride. An allylthio group as a pharmacologically active group was introduced into one side of a pyridazine ring. Arylalkylamines with benzene or pyridine moieties or heterocycloalkylamines with heterocycle moieties such as morpholine, piperidine, or pyrrolidine were also introduced into the para-position of allylthio pyridazine. These new compounds showed antiproliferative activities against SK-Hep-1 human liver cancer cells in MTT assays. These compounds are thus promising candidates for chemotherapy of hepatocellular carcinomas. Two compounds, 20c and 22a, showed higher potencies for inhibiting growth of hepatocellular carcinoma cells than did K6 ($ID_50$=1.08 mM). This suggests the potential anticancer activity of these two compounds.

• Bulletin of the Korean Chemical Society
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• 제34권5호
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• pp.1487-1493
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• 2013

Based on the finding that the 2-aminobenzamido group of MS-275 plays a crucial role in inhibiting HDACs through chelation of zinc existing at the active site of HDAC enzymes, novel N-(2-hydroxyphenyl)arylsulfonamide derivatives were synthesized for their potential ability to inhibit HDACs and evaluated for anticancer activity against human breast cancer cell line (MCF-7). Although the synthesized arylsulfonamides have failed to significantly inhibit total HDACs activity, phenyl carbamate-linked arylsulfonamide 10 and benzyl thiocarbamate-linked arylsulfonamide 15 exhibited good anticancer activities, which were only 4.3- and 3.6-fold lower anticancer activities, respectively, than MS-275 that is undergoing phase II clinical trials. These results suggest that these compounds may act as a selective HDAC inhibitor and probably N-(2-hydroxyphenyl) sulfamoyl group may play an important role in interacting with HDAC enzymes through chelation of zinc ion.

• Archives of Pharmacal Research
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• 제24권4호
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• pp.276-280
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• 2001

Substituted isoquinolin-1-ones (1) were synthesized to test their in vitro anticancer activity. 3-Biphenyl-H-methylisoquinolin-1-one (7) showed the most potent anticancer activity against five different human cancer cell lines.

• Bulletin of the Korean Chemical Society
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• 제32권spc8호
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• pp.3009-3016
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• 2011

To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.

• Journal of Microbiology and Biotechnology
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• 제24권3호
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• pp.346-353
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• 2014

The chlorophyll-related compound pheophorbide a (Pa) was successively purified from an edible red seaweed, Grateloupia elliptica, using silica, octadecyl silica column chromatography and reversed phase-high-performance liquid chromatography, as well as the cell cycle inhibitory and apoptotic effects of Pa being investigated in U87MG glioblastoma cells. The Pa exhibited strong anticancer effects in the absence of direct photo-irradiation against various cancer cell lines, including U87MG, SK-OV-3, and HeLa cells. Among the cancer cells, the strongest anticancer activity of Pa exhibited on U87MG cells with $IC_{50}$ values of 2.8 ${\mu}g/ml$. In addition, Pa specifically had cytostatic activity on glioblastoma cells rather than human umbilical vein endothelial cells. Analysis of the cell cycle distribution showed that Pa induced G0/G1 arrest of U87 MG cells. In addition, arrested cells induced late apoptosis and DNA degradation under dark condition. These results suggest that Pa isolated from G. elliptica is a potential glioblastoma-specific anticancer agent without side effects on normal cells.

• 대한수의학회지
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• 제62권1호
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• pp.3.1-3.7
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• 2022

Disulfiram (DSF) is a marketed drug to treat patients with alcohol dependence by inhibiting aldehyde dehydrogenase. Over the last few decades, DSF has been shown to have anticancer effects through different mechanisms. Moreover, this effect can be elevated when used with copper (Cu). Subsequent studies have been conducted on various cancers, but few on lymphoma. This study investigated the anticancer effects of DSF on lymphoma and how this effect changed when treated with Cu. DSF synergistically decreased the metabolic activity of EL4 lymphoma cells when combined with Cu. At 1 µM of DSF alone, the metabolic activity of EL4 cells decreased by 49% compared to the control, whereas it decreased by 87% with a DSF + CuCl₂ treatment. Rhodamine 123 and 2',7'-dichlorofluorescein diacetate staining showed that DSF induced the reduction of the mitochondrial membrane potential and promoted the production of reactive oxygen species. In particular, the combined treatment of DSF + Cu induced cell death based on multiple assays, including annexin V-fluorescein isothiocyanate/propidium iodide staining. Overall, DSF has anticancer effects on lymphoma cells and exhibits synergistic effects when combined with Cu. This study provides some valuable information to broaden the use of DSF in clinics and basic research.

• 한국육종학회지
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• 제43권4호
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• pp.297-303
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• 2011

종피색이 다른 세 품종을 이용하여 총페놀함량, 항산화활성 및 항암활성의 변이를 조사하였다. 총페놀함량은 흑진주벼의 쌀겨와 영이 적진주벼와 일품벼보다 높게 나타났으며, 흑진주에서는 쌀겨가 영보다 함량이 높았으나 다른 두 품종은 영이 쌀겨보다 함량이 높았다. DPPH 자유기 소거능은 흑진주와 적진주의 활성이 일품벼 보다 높았으며, 쌀겨 추출물이 영 추출물보다 훨씬 높은 활성을 보였다. 환원력은 흑진주의 쌀겨 추출물이 다른 품종의 쌀겨 추출물보다 3~16배의 높은 활성을 보였으며, 적진주와 일품에서는 영 추출물의 활성이 쌀겨 추출물보다 높았다.$ABTS^+$ 라디컬 소거능은 일품벼의 영 추출물이 가장 높은 활성을 보였으며, 세 품종에서 모두 영 추출물이 쌀겨 추출물 보다 높은 활성을 보였다. HepG2 cell에 대한 항암활성 검정 결과, 쌀겨 추출물보다 영 추출물의 항암활성이 평균적으로 20% 정도 높게 나타났으며, 적진주벼와 일품벼의 영 추출물은 92% 정도의 유사한 활성을 보였고, 흑진주벼는 30.4%의 낮은 활성을 보였다. 벼 영 추출물의 항암활성은 총페놀함량, PDDH 자유기 소거능, 그리고 환원력과 유의한 정의 상관을 보였으나 쌀겨 추출물은 페놀함량이나 항산화 활성과 유의한 상관관계가 없었다. 결론적으로, 벼의 쌀겨와 왕겨는 강력한 항산화 및 항암 활성을 보였으며, 종피색이 다른 3가지 벼 품종에서 총페놀함량, 항산화 활성, 그리고 항암활성의 변이를 나타내었다.

• 약학회지
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• 제17권3호
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• pp.147-151
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• 1973

Fifteen thiosemicarbazone derivatives were synthesized and evaluated for their antimicrobial activity against Staphylococus aureus, Escherchia coli and Pichia sp. Anticancer activity in vitro was also tested against human carcinoma HeLa cells.