• Archives of Pharmacal Research
• /
• v.29 no.10
• /
• pp.826-833
• /
• 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
• /
• v.5 no.1
• /
• pp.54-57
• /
• 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
• /
• v.30 no.1
• /
• pp.83-91
• /
• 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
• /
• v.34 no.5
• /
• pp.1487-1493
• /
• 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
• /
• v.24 no.4
• /
• pp.276-280
• /
• 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
• /
• v.32 no.spc8
• /
• pp.3009-3016
• /
• 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
• /
• v.24 no.3
• /
• pp.346-353
• /
• 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.

• Korean Journal of Veterinary Research
• /
• v.62 no.1
• /
• pp.3.1-3.7
• /
• 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.

• Korean Journal of Breeding Science
• /
• v.43 no.4
• /
• pp.297-303
• /
• 2011

In order to confirm the biological activities of rice bran and hull, total phenolic content, antioxidant and anticancer activities were examined in three rice varieties that have different seed coat colors such as brown, black, and purple. The antioxidant activity was measured by free radical scavenging assay including DPPH, $ABTS^+$ and reducing power activity. The anticancer activity was evaluated by WST assay with human HepG2 cell lines. As the result, Huegjinju, black seed coat rice, showed higher of the total phenolics contents in both bran and hull, than purple Jeojinju and brown Ilpum. In the antioxidant activity, Heugjinju showed the highest among the bran extracts, but the activities of hull extracts were similar in three varieties. In the anticancer activity to HepG2 cell line, the hull extract was 20% higher than that of bran extract in the average of three varieties. The hull extracts of Ilpum and Jeokjinju showed similar anticancer activites about 92%, and that of Heugjinju showed the lowest activity of 30.4%. The anticancer activities of hull extracts in three varieties showed positive correlation with total phenolics contents, DPPH radical scavenging activities and reducing power activities. In conclusion, the rice bran and hull showed potent antioxidant and anticancer activities varied in three varieties that have different seed coat colors.

• YAKHAK HOEJI
• /
• v.17 no.3
• /
• pp.147-151
• /
• 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.