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carboxylic acid/sarcoma
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Interaction of 2-aminobicyclo[3.2.1]octane-2-carboxylic acid with the amino acid transport systems of the sarcoma 37 murine ascites tumor cell.
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The relatively broad and overlapping specificities of amino acid transport systems have made the synthesis of analogues specific to single transport systems desirable. The analogue in general use as a specific substrate for transport system L has been 2-aminobicyclo[2.2.1]heptane-2-carboxylic acid
High-resolution structure of the catalytic domain of avian sarcoma virus integrase.
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Retroviral integrase (IN) functions to insert retroviral DNA into the host cell chromosome in a highly coordinated manner. IN catalyzes two biochemically separable reactions: processing of the viral DNA ends and joining of these ends to the host DNA. Previous studies suggested that these two
Synthesis, Radiolabeling, and Biological Evaluation of the Cis Stereoisomers of 1-amino-3-(fluoro- 18 F)-4-fluorocyclopentane-1-carboxylic acid as PET Imaging Agents
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The non-natural cyclic amino acids (1S,3R,4S)-1-amino-3-fluoro-4-(fluoro-<sup><i>18</sup>F</i>)cyclopentane-1-carboxylic acid ([<sup><i><b>18</sup>F</i>]9</b>) and
Differential expression and functional characterization of system L amino acid transporters in human normal osteoblast cells and osteogenic sarcoma cells.
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BACKGROUND
The amino acid transport system L is a major nutrient transport system responsible for Na(+)-independent transport of neutral amino acids, including several essential amino acids. The system L is divided into two major subgroups, the L-type amino acid transporter 1 (LAT1) and the L-type
4-Methyl-1,2,3-selenadiazole-5-carboxylic acid amides: antitumor action and cytotoxic effect correlation.
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Synthesis and cytotoxic activity of a series of 4-methyl-1,2,3-selenadiazole-5-carboxylic acid amides on human fibrosarcoma HT-1080, mouse hepatoma MG-22A, and mouse fibroblasts 3T3 cell lines are described. The correlation between compound LD(50) and 3T3 fibroblast cell line morphology was shown.
Anionic polymers and biological activities. Effects of some new polycarboxylic acids on the ascitic sarcoma 180 in mice.
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Eleven new polymeric carboxylic acids with widely different solubilities in water have been synthesized. The activities of these polymers against the ascitic sarcoma 180 tumor of mice and their acute toxicities in mice have been compared with molecular parameters of the polymers such as molecular
Broad-spectrum antiviral activity and mechanism of antiviral action of the fluoroquinolone derivative K-12.
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The fluoroquinolone derivatives have been shown to inhibit human immunodeficiency virus (HIV) replication at the transcriptional level. We confirmed the anti-HIV activity of the most potent congener, 8-difluoromethoxy-1-ethyl-6-fluoro-1,4-dihydro-7-[4-(2-
Influence of photoinitiator concentration and irradiation time on the crosslinking performance of visible-light activated pullulan-HEMA hydrogels.
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In-situ forming hydrogels were prepared from pullulan-HEMA copolymer using three-component visible-light system composed of camphorquinone carboxylic acid-folic acid-iodonium salt. The relevance of double bond conversion and crosslinking density of hydrogels with the photoinitiator concentration and
Phase I toxicologic study of Lonidamine in cancer patients.
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15 patients with metastatic cancer were treated with Lonidamine, a substituted indazole carboxylic acid active against the Lewis lung and Sarcoma 180 tumors. Single doses of 600 mg (350-400 mg/m2) mostly induced somnolence and gastro-intestinal side effects. Toxicity occurring during chronic
Inhibition of Chronic Pancreatitis and Murine Pancreatic Intraepithelial Neoplasia by a Dual Inhibitor of c-RAF and Soluble Epoxide Hydrolase in LSL-KrasG¹²D/Pdx-1-Cre Mice.
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Mutation of Kirsten rat sarcoma viral oncogene homolog (KRAS) and chronic pancreatitis are the most common pathogenic events involved in human pancreatic carcinogenesis. In the process of long-standing chronic inflammation, aberrant metabolites of arachidonic acid play a crucial role in promoting
The secalosides, novel tumor cell growth inhibitory glycosides from a pollen extract.
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The pollen of rye (Secale cereale) was shown to contain a biologically highly active family of glycosides called the secalosides. Secalosides A and B (1), both of molecular formula C46H51-NO24, were found to be epimeric esters of (2-oxo-3-indolyl)acetic acid (4). They are made up, in addition to
Collagen-production inhibitors evaluated as antitumor agents.
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Proline analogues such as cis-4-hydroxy-L-proline (CHP) and L-azetidine-2-carboxylic acid (A2C) were tested for their antitumor activity in tissue culture and in vivo. In culture, CHP specifically inhibited those tumor cells that synthesized basement-membrane collagen. CHP appeared to selectively
Phase II evaluation of Lonidamine in patients with advanced malignancy.
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Lonidamine, a substituted indazole carboxylic acid with unique effects on cellular respiration, was studied in 27 patients with advanced malignancies. Of the 18 evaluable patients, 5 had small-cell lung cancer, 3 had non-small-cell lung cancer, 3 sarcoma, 2 breast cancer, and 5 other tumour types.
[Synthesis and antitumor action of N,N-di(2-chlorethyl)-hydrazines of alpha-aminocarboxylic acid antimetabolites].
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The N,N-di(2-chlorethyl)hydrazides of the following alpha-aminocarboxylic acid antimetabolites: methioninsulphoxide, ethionine, 2-, 3- and 4-fluorophenylalanine, 4-nitrophenylalanine and 2,2-dimethyl-thiazolidine-4-carboxylic acid were synthesized. Preliminary studies of the activity on experimental
In vitro studies on the metabolism of trabectedin (YONDELIS) in monkey and man, including human CYP reaction phenotyping.
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Trabectedin (YONDELIS) is a potent anticancer agent which was recently approved in Europe for the treatment of soft tissue sarcoma. The drug is currently also in clinical development for the treatment of ovarian carcinoma. In vitro experiments were conducted to investigate the hepatic metabolism of
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