Search Results - "Stinson, Sherman F."
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Antitumor Benzothiazoles. 8. Synthesis, Metabolic Formation, and Biological Properties of the C- and N-Oxidation Products of Antitumor 2-(4-Aminophenyl)benzothiazoles
Published in Journal of medicinal chemistry (07-10-1999)“…2-(4-Aminophenyl)benzothiazoles 1 and their N-acetylated forms have been converted to C- and N-hydroxylated derivatives to investigate the role of metabolic…”
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2
FLUORINATED 2-(4-AMINO-3-METHYLPHENYL)BENZOTHIAZOLES INDUCE CYP1A1 EXPRESSION, BECOME METABOLIZED, AND BIND TO MACROMOLECULES IN SENSITIVE HUMAN CANCER CELLS
Published in Drug metabolism and disposition (01-12-2004)“…Fluorinated 2-(4-amino-3-methylphenyl)benzothiazoles possess potent antiproliferative activity against certain cancer cells, similar to the unfluorinated…”
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17-(Allylamino)-17-demethoxygeldanamycin activity in human melanoma models
Published in Anti-cancer drugs (01-04-2004)“…17-(Allylamino)-17-demethoxygeldanamycin (17-AAG) is a semisynthetic antitumor agent, which has entered phase I/II clinical trials. Melanoma cell lines in the…”
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Optimization of Naphthalimide-imidazoacridone with Potent Antitumor Activity Leading to Clinical Candidate (HKH40A, RTA 502)
Published in Journal of medicinal chemistry (15-11-2007)“…Unsymmetrical bifunctional antitumor agent WMC79 was further optimized to generate compound 7b that not only inhibited the growth of many tumor cell lines, but…”
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Anti-tumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces single-strand breaks and DNA-protein cross-links in sensitive MCF-7 breast cancer cells
Published in Cancer chemotherapy and pharmacology (01-07-2006)“…The fluorinated benzothiazole analogue 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) exhibits selective and potent anticancer activity,…”
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Preclinical evaluation of amino acid prodrugs of novel antitumor 2-(4-amino-3-methylphenyl)benzothiazoles
Published in Molecular cancer therapeutics (01-02-2002)“…Novel 2-(4-aminophenyl)benzothiazoles (e.g., compounds 1 and 2) possess highly selective, potent antitumor properties in vitro and in vivo. Elucidation of the…”
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The antitumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces NF-κB activity in drug-sensitive MCF-7 cells
Published in Anti-cancer drugs (01-02-2005)“…2-(4-Amino-3-methylphenyl)-5-fluoro-benzothiazole (5F 203) potently inhibits MCF-7 breast cancer cell growth in part by activating the aryl hydrocarbon…”
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8
Synthesis, structure-activity relationship, and p210(bcr-abl) protein tyrosine kinase activity of novel AG 957 analogs
Published in Bioorganic & medicinal chemistry (01-03-2005)“…A series of novel, sterically hindered lipophilic analogs of AG 957 was designed and synthesized as potential protein tyrosine kinase (PTK) inhibitors. The in…”
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Clinical Pharmacology of Flavopiridol Following a 72-Hour Continuous Infusion
Published in The Annals of pharmacotherapy (01-10-2003)“…Background Flavopiridol, a novel flavone derivative, inhibits cyclin-dependent kinase-1. We initiated a Phase I trial in patients with refractory solid tumors…”
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Poly(ethylene glycol) Prodrugs of the CDK Inhibitor, Alsterpaullone (NSC 705701): Synthesis and Pharmacokinetic Studies
Published in Bioconjugate chemistry (01-09-2004)“…Two methods were devised to conjugate PEG to alsterpaullone (NSC 705701) via the N of the indole ring portion of the molecule. In the first approach,…”
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Identification of cytosolic aldehyde dehydrogenase 1 from non-small cell lung carcinomas as a flavopiridol-binding protein
Published in FEBS letters (02-07-1999)“…The synthetic flavone flavopiridol can be cytostatic or cytotoxic to mammalian cells, depending on the concentration of the drug and the duration of exposure…”
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Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: Differential accumulation and metabolism
Published in Biochemical pharmacology (01-06-1999)“…The tricyclic compound 2,5-bis(5-hydroxymethyl-2-thienyl)furan (NSC 652287) has shown a highly selective pattern of differential cytotoxic activity in the…”
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13
Multidrug-resistant phenotype of disease-oriented panels of human tumor cell lines used for anticancer drug screening
Published in Cancer research (Chicago, Ill.) (01-06-1992)“…Disease-oriented panels of human tumor cell lines used by the National Cancer Institute for large-scale in vitro anticancer drug screening were evaluated for…”
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14
Identification of the major metabolite of 2,5-bis(5-hydroxymethyl-2-thienyl)furan (NSC 652287), an antitumor agent, in the S9 subcellular fraction of dog liver cells
Published in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences (05-02-2002)“…α-Terthienyl ( 1) is a trithiophene found widely distributed in plants. Other naturally occurring trithiophenes are less widely distributed, but nonetheless…”
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Preclinical evaluation of 9-chloro-2-methylellipticinium acetate alone and in combination with conventional anticancer drugs for the treatment of human brain tumor xenografts
Published in Journal of cancer research and clinical oncology (01-01-1998)“…Some ellipticine derivative salts, including 9-chloro-2-methylellipticinium (CME), have been found to have a marked selectivity against all eight brain tumor…”
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Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms
Published in Journal of clinical oncology (01-09-1998)“…We conducted a phase I trial of the cyclin-dependent kinase inhibitor, flavopiridol (National Service Center [NSC] 649890), to determine the maximum-tolerated…”
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Multifactorial hamster respiratory carcinogenesis with interdependent effects of cannula-induced mucosal wounding, saline, ferric oxide, benzo[a]pyrene and N-methyl-N-nitrosourea
Published in Cancer research (Chicago, Ill.) (15-03-1989)“…The carcinogenic response induced in the respiratory tract of Syrian golden hamsters by repeated intratracheal instillations of benzo[a]pyrene (BP) adsorbed to…”
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Morphological and cytokinetic responses of hamster airways to intralaryngeal or intratracheal cannulation with instillation of saline or ferric oxide particles in saline
Published in Cancer research (Chicago, Ill.) (15-03-1989)“…The morphological and proliferative effects of intratracheal cannulation (ITC) or intralaryngeal cannulation (ILC), with or without the instillation of saline…”
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Role of CYP1A1 in modulation of antitumor properties of the novel agent 2-(4-amino-3-methylphenyl)benzothiazole (DF 203, NSC 674495) in human breast cancer cells
Published in Cancer research (Chicago, Ill.) (15-09-2000)“…2-(4-Amino-3-methylphenyl)benzothiazole (DF 203, NSC 674495) is a candidate antitumor agent with potent and selective activity against human-derived tumor cell…”
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Flavopiridol Induces Apoptosis of Normal Lymphoid Cells, Causes Immunosuppression, and Has Potent Antitumor Activity In Vivo Against Human Leukemia and Lymphoma Xenografts
Published in Blood (01-04-1998)“…Flavopiridol is a novel semisynthetic flavone derivative of the alkaloid rohitukine. Flavopiridol is known to inhibit potently the activity of multiple…”
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