Search Results - "EHLHARDT, W. J"

Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979 by DANTZIG, A. H, SHEPARD, R. L, CAO, J, LAW, K. L, EHLHARDT, W. J, BAUGHMAN, T. M, BUMOL, T. F, STARLING, J. J

“…Overexpression of P-glycoprotein (Pgp) by tumors results in multidrug resistance (MDR) to structurally unrelated oncolytics. MDR cells may be sensitized to…”
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Sulfonimidamide analogs of oncolytic sulfonylureas by TOTH, J. E, GRINDEY, G. B, WEIR, L. C, WORZALLA, J. F, EHLHARDT, W. J, RAY, J. E, BODER, G. B, BEWLEY, J. R, KLINGERMAN, K. K, GATES, S. B, RINZEL, S. M, SCHULTZ, R. M

“…A series of sulfonimidamide analogs of the oncolytic diarylsulfonylureas was synthesized and evaluated for (1) in vitro cytotoxicity against CEM cells, (2) in…”
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Metabolism and Disposition of the Antifolate LY231514 in Mice and Dogs by WOODLAND, J. M, BARNETT, C. J, DORMAN, D. E, GRUBER, J. M, SHIH, C, SPANGLE, L. A, WILSON, T. M, EHLHARDT, W. J

“…The metabolism and disposition of LY231514 was studied in mice and dogs. LY231514 is a novel pyrrolopyrimidine-based multi-target antifolate (MTA) showing…”
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Metabolism and disposition of the anticancer agent sulofenur in mouse, rat, monkey, and human by Ehlhardt, W J

“…The elimination and metabolism of sulofenur [N-(5-indanesulfonyl)-N'-(4-chlorophenyl)urea, LY186641] was examined in mice, rats, monkeys, and humans. The…”
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Metabolism and disposition of p-chloroaniline in rat, mouse, and monkey by Ehlhardt, W J, Howbert, J J

“…The metabolism and disposition of [14C]p-chloroaniline was studied in the male Fisher 344 rat, female C3H mouse, and male rhesus monkey. Greater than 90% of…”
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Liquid Chromatography/Nuclear Magnetic Resonance Spectroscopy and Liquid Chromatography/Mass Spectrometry Identification of Novel Metabolites of the Multidrug Resistance Modulator LY335979 in Rat Bile and Human Liver Microsomal Incubations by EHLHARDT, W. J, WOODLAND, J. M, BAUGHMAN, T. M, VANDENBRANDEN, M, WRIGHTON, S. A, KROIN, J. S, NORMAN, B. H, MAPLE, S. R

“…Compound LY335979 is a P-glycoprotein inhibitor currently entering phase I clinical trials for potential reversal of multidrug resistance to cancer…”
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Characterization of an O-glucuronide metabolite of the CCK-B antagonist LY288513 and its plasma levels in mouse, rat, and dog by Woodland, J M, Ehlhardt, W J

“…LY288513 [(4S,5R)-trans-N-(4-bromophenyl)-3-oxo-4,5-diphenyl-1- pyrazolidinecarboxamide] has been developed as a cholecystokinin-B antagonist for anxiolytic…”
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Biotransformation of the antiviral agent 1,3,4-thiadiazol-2-ylcyanamide (LY217896) and characteristics of a mesoionic ribose metabolite by Ehlhardt, W J, Wheeler, W J, Breau, A P, Chay, S H, Birch, G M

“…The biotransformation of the antiinfluenza agent 1,3,4-thiadiazol-2-ylcyanamide (LY217896, I) was studied. In addition to a urea metabolite (II) formed by…”
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Disposition and metabolism of the Sulfonylurea Oncolytic Agent LY295501 in Mouse, Rat, and Monkey by EHLHARDT, W. J, WOODLAND, J. M, TOTH, J. E, RAY, J. E, MARTIN, D. L

“…The disposition and metabolism of LY295501 was studied in mice, rats, and monkeys. This novel diaryl sulfonylurea oncolytic agent is structurally related to…”
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Formation of indenesulfonylureas in the metabolism of the anticancer agent sulofenur in rats, monkeys, and humans by Ehlhardt, W J, Zimmermann, J L, Ray, J E, Toth, J E

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Metabolism of Capsaicin by Cytochrome P450 Produces Novel Dehydrogenated Metabolites and Decreases Cytotoxicity to Lung and Liver Cells by Reilly, Christopher A, Ehlhardt, William J, Jackson, David A, Kulanthaivel, Palaniappan, Mutlib, Abdul E, Espina, Robert J, Moody, David E, Crouch, Dennis J, Yost, Garold S

“…Capsaicin is a common dietary constituent and a popular homeopathic treatment for chronic pain. Exposure to capsaicin has been shown to cause various…”
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Thiol-mediated incorporation of radiolabel from 1-[14C]-methyl-4-phenyl-5-nitrosoimidazole into DNA. A model for the biological activity of 5-nitroimidazoles by Ehlhardt, W J, Goldman, P

“…1-Methyl-4-phenyl-5-nitrosoimidazole (5NO), which has properties consistent with the biologically active form of a 5-nitroimidazole, was radiolabeled…”
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Comparison of metabolism and toxicity to the structure of the anticancer agent sulofenur and related sulfonylureas by Ehlhardt, William J, Woodland, Joseph M, Worzalla, John F, Bewley, Jesse R, Grindey, Gerald B, Todd, Glen C, Toth, John E, Howbert, J. Jeffry

“…The metabolic formation of p-chloroaniline from the oncolytic agent sulofenur [N-(5-indanesulfonyl)-N'-(4-chlorophenyl)urea, LY186641,] and from similar…”
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Pharmacokinetics of the anticancer agent sulofenur in mice, rats, monkeys, and dogs by Ehlhardt, W J, Sullivan, H R, Wood, P G, Woodland, J M, Hamilton, M, Hamilton, C, Cornpropst, D, Grindey, G B, Worzalla, J F, Bewley, J R

“…The absorption and pharmacokinetics of sulofenur [N-(indan-5-sulfonyl)-N'-(4-chlorophenyl)urea, LY186641] and its major metabolites were examined in mice,…”
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Formation of an amino reduction product of metronidazole in bacterial cultures: lack of bactericidal activity by Ehlhardt, W J, Beaulieu, Jr, B B, Goldman, P

“…To investigate whether the amino reduction product of metronidazole has antibacterial activity, 5-amino-1-beta-hydroxyethyl-2-methylimidazole (AMN) was…”
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Glutathione-Dependent Metabolism of the Antitumor Agent Sulofenur. Evidence for the Formation of p-Chlorophenyl Isocyanate as a Reactive Intermediate by Jochheim, Claudia M, Davis, Margaret R, Baillie, Kathleen M, Ehlhardt, William J, Baillie, Thomas A

“…The antitumor agent sulofenur (LY186641), which has shown promising activity against a wide range of cancers, causes hemolytic anemia and methemoglobinemia at…”
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Mammalian cell toxicity and bacterial mutagenicity of nitrosoimidazoles by Ehlhardt, W J, Beaulieu, Jr, B B, Goldman, P

“…It is currently believed that the biological activity of such therapeutic 5-nitroimidazoles as metronidazole is mediated by a short-lived, highly toxic species…”
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Chemical and biological properties of acetyl derivatives of the hydroxylamino reduction products of metronidazole and dimetridazole by Ehlhardt, W J, Beaulieu, Jr, B B, Goldman, P

“…Metronidazole and related 5-nitroimidazoles undergo reduction of their nitro group apparently to produce such reactive species as 5-hydroxylaminoimidazoles. To…”
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Binding of the epoxide cryptophycin analog, LY355703 to albumin and its effect on in vitro antiproliferative activity by Schultz, R M, Shih, C, Wood, P G, Harrison, S D, Ehlhardt, W J

“…Cryptophycin, isolated from the cyanobacterium Nostoc, is a cytotoxic dioxadiazacyclohexadecenetetrone which causes rapid depletion of microtubules in intact…”
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Novel acid labile COL1 trityl-linked difluoronucleoside immunoconjugates: synthesis, characterization, and biological activity by Patel, V F, Hardin, J N, Mastro, J M, Law, K L, Zimmermann, J L, Ehlhardt, W J, Woodland, J M, Starling, J J

“…LY207702 (1) is a difluorinated purine nucleoside that exhibits impressive antitumor activity in preclinical models. This agent, however, also possesses…”
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