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Fli-1 Activation through Targeted Promoter Activity Regulation Using a Novel 3', 5'-diprenylated Chalcone Inhibits Growth and Metastasis of Prostate Cancer Cells.
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The friend leukemia integration 1 (Fli-1) gene is involved in the expression control of key genes in multiple pathogenic/physiological processes, including cell growth, differentiation, and apoptosis; this implies that Fli-1 is a strong candidate for drug development. In our previous study, a
Effect of trichloropropene oxide on the ability of polyaromatic hydrocarbons and their "K-region" oxides to initiate skin tumors in mice and to bind to DNA in vitro.
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The potent epoxide hydrase inhibitor, 1,1,1-trichloro-2,3-propene oxide (TCPO), enhanced the tumor-initiating ability of benzo[alpha]pyrene (BP) and 3-methylcholanthrene (MCA) but had no effect on 9,10-dimethyl-1,2-anthracene (DMBA) initiation in a two-stage system of tumorigenesis in female Charles
Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. III. Synthesis and antitumor activity of 3-phenylpiperazinyl-1-trans-propenes.
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A series of novel 3-[4-phenyl-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes and related compounds were synthesized and evaluated by their cytotoxic activity against several tumor cell lines in vitro and in vivo antitumor activity against some tumor models when
Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. II. Optimization of the phenylpiperazine moiety of 1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes.
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A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propene (2) were synthesized and evaluated by
Anti-tumor-promoting effects of phenylpropanoids on Epstein-Barr virus activation and two-stage mouse skin carcinogenesis.
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In our joint project in the search for anti-tumor promoters from natural plant sources, we carried out a primary screening of 12 phenylpropanoids isolated from Boronia pinnata Sm. (Rutaceae) by examining their possible inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation
[Studies on constituents of rootsanel leaves from Desmodium blandum and their cytotoxic activity against growth of several tumor cells].
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OBJECTIVE
To investigate the chemical constituents of Desmodium blandum and their cytotoxic activity against the growth of several tumor cells.
METHODS
Various chromatographic techniques including silica gel, Sephadex LH-20 column chromatography were employed for the isolation and purification of
Ex vivo emission of volatile organic compounds from gastric cancer and non-cancerous tissue.
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The presence of certain volatile organic compounds (VOCs) in the breath of patients with gastric cancer has been reported by a number of research groups; however, the source of these compounds remains controversial. Comparison of VOCs emitted from gastric cancer tissue to those emitted from
Targeted Smart pH and Thermoresponsive N,O-Carboxymethyl Chitosan Conjugated Nanogels for Enhanced Therapeutic Efficacy of Doxorubicin in MCF-7 Breast Cancer Cells.
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In cancer treatment, developing ideal anticancer drug delivery systems to target tumor microenvironment by circumventing various physiological barriers still remains a daunting challenge. Here, in our work, a series of pH- and temperature-responsive nanogels based on
Anti-cancer chalcones: Structural and molecular target perspectives.
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Chalcone or (E)-1,3-diphenyl-2-propene-1-one scaffold remained a fascination among researchers in the 21st century due to its simple chemistry, ease of synthesis and a wide variety of promising biological activities. Several natural and (semi) synthetic chalcones have shown anti-cancer activity due
Intestinal bacteria and endogenous production of malonaldehyde and alkylators in mice.
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Association of intestinal bacteria with endogenous production of some reactive compounds was studied by determination of adducts to haemoglobin in blood from germ-free and corresponding control mice. N-terminal valines in haemoglobin were analysed with regard to adducts from malonaldehyde (MA),
NTP Toxicology and Carcinogenesis Studies of Methyleugenol (CAS NO. 93-15-2) in F344/N Rats and B6C3F1 Mice (Gavage Studies).
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Methyleugenol is used as a flavoring agent in jellies, baked goods, nonalcoholic beverages, chewing gum, candy, pudding, relish, and ice cream. It is also used as a fragrance in perfumes, creams, lotions, detergents, and soaps. Methyleugenol has also been used as an insect attractant in eradication
NTP Toxicology and Carcinogenesis Studies of 3-Chloro-2-methylpropene (Technical grade containing 5% dimethylvinyl chloride) (CAS No. 563-47-3) in F344/N Rats and B6C3F1 Mice (Gavage Studies).
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Toxicology and carcinogenesis studies of technical-grade 3-chloro-2-methylpropene (containing 5% dimethylvinyl chloride), a widely used insecticide and a chemical intermediate, were performed on F344/N rats and B6C3F1 mice. In the 13-week studies, 50%-100% mortality occurred in groups of male and
Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives.
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Novel pyrimidinyl pyrazole derivatives were synthesized and examined for cytotoxic and antitumor activity. Mannich reaction was employed to construct this scaffold. Among the compounds synthesized, a series of propene derivatives exhibited a potent cytotoxic activity against some tumor cell lines
Garlicnins B(1), C(1), and D, from the fraction regulating macrophage activation of Allium sativum.
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Several novel sulfides from acetone extracts of bulbs of garlic (Allium sativum L.), were identified and investigated. These were named garlicnins B(1) (1), C(1) (2), and D (3), and they were found to have the ability to control macrophage activation. Garlicnins B(1) (1) and C(1) (2) possess a new
[Tridentate N-N-N chelating systems as potential antitumor agents].
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Tridentate chelating agents, as potential antitumor agents, were prepared by condensing 2-quinolylhydrazines, 2-pyridylhydrazine and 2-benzothiazolylhydrazine with pyridine-2-aldehyde, 6-methylpyridine-2-aldehyde, 2-acetylpyridine and 2-benzoylpyridine. All compounds were tested against Lymphocytic
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