ABSTRACT: Substituted isoquinolin-1-ones (1) were synthesized to test theirin vitro anticancer activity. 3-Biphenyl-N-methylisoquinolin-1-one (7) showed the most potent anticancer activity against five different human cancer cell lines.
Archives of Pharmacal Research 04/2012; 24(4):276-280. · 1.59 Impact Factor
ABSTRACT: Doxorubicin, one of the clinically most useful anticancer agents, is used alone or in combination with other drugs against
a wide variety of tumors, recently. But cancer cells developed resistance to this agent in many ways. This resistance is an
important limiting factor of doxorubicin for anticancer drug. We newly established doxorubicin-resistant HCT15/CL02 subline
from parental HCT15 human adenocarcinoma colon cancer cells. HCT15/CL02 revealed resistance to doxorubicin about 85-fold of
its parental cells, and it also revealed cross-vealed to actinomycin D, etoposide and vinblastine but not to cisplatin and
tamoxifen. And verapamil, a reversal agent of multidrug-resistance (MDR) by P-glycoprotein, elevated the cytotoxicity of doxorubicin
against both HCT15 and HCT15/CL02 cells. But the relative resistant rate was not reduced. Verapamil had no effects on the
toxicity of cisplatin to the both cell lines. These results indicate that HCT15/CL02 cells have some functionally complex
mechanisms for MDR.
Archives of Pharmacal Research 09/1996; 19(5):342-347. · 1.59 Impact Factor
ABSTRACT: Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various
purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BP002-A) was isolated from the fermentation broth ofAspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition
of cell growthin vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system
cancer cell XF498 were 8.24, 10.60, 8.83, 9.85 μg/ml respectively. GERI-BP002-A has also revealed cytotoxicity against P-glycoprotein-expressed
human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein.
We have also tested cytotoxicities of structurally related compounds of GERI-BP002-A such as diphenylmethane, 1,1-bis(3,4-dimethylphenyl)ethane,
2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, 4,4′-di-tert-butylphenyl, bibenzyl, 2,2′-dimethylbibenzyl,cis-stilbene,trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenylsulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship,
and from these data we could suppose that hydroxyl group of GERI-BP002-A conducted important role in its cytotoxicity.
Archives of Pharmacal Research 04/1996; 19(4):286-291. · 1.59 Impact Factor
ABSTRACT: The trichothecenes are sesquiterpenoid mycotoxins characterized by the 12,13-epoxytrichothec-9-ene ring system. We have tested
cytotoxicity of several naturally-occurring or synthesized trichothecenes against human solid tumor cell lines. Among them,
trichothecin (I) and 4-β-Acetoxy-12,13-epoxytrichothec-9-ene (trichodermin, II) exhibited highly cytotoxic activities. 4-β-Hydroxy-12,13-epoxytrichothec-9-ene
(trichodermol, III) and 4-β-Methoxy-12,13-epoxytrichothec-9-ene and 4-α-Hydroxy-12,13-epoxytrichothec-9-ene(VI) had no cytotoxicities
up to 10 μg/ml. And in the tested cell lines, HCT15 colon cancer cell line was the most sensitive to all tested trichothecenes.
Archives of Pharmacal Research 04/1996; 19(1):6-11. · 1.59 Impact Factor
ABSTRACT: Design and synthesis of novel 4-phenyl-1-arylsulfonylimidazolones3 and 4-phenyl-3-arylsulfonylimidazolones4 and evaluation of their cytotoxic activity against eleven human cancer cell lines and two murine leukemia cell linesin vitro were performed. As a result, a series of 4-phenyl-1(N)-arylsulfonylimidazolones (3) has been found to be the potential anticancer agent. Compounds3b, 3c, and3d exhibit strong activity as indicated by their IC50 values 0.39, 3.19, 0.31 μg/mL against A549 and 0.80, 0.48, 0.0007 μg/mL against SK-Mel-2, respectively. These compounds also
possess much more potent activity (10–1000 times) than LY186641 against eleven other cell lines.
Archives of Pharmacal Research 01/1996; 19(6):570-580. · 1.59 Impact Factor
Bioorganic & Medicinal Chemistry Letters. 6(21):2553-2558.