Zobrazeno 1 - 10
of 23
pro vyhledávání: '"William J. Ehlhardt"'
Autor:
Mark Edward Rempala, Tom Raub, Carlos Mateos, Sehila Pleite, Josh Clayton, William J. Ehlhardt, Huaxing Pei, Bradley Condon, Stephanie L. Stout, Sheela Ashok, Sandaruwan Geeganage, Mei Lai, Burkholder Timothy P, Deidre Michelle Johns, Yong Wang, Kenneth James Junior Henry, Saravanan Parthasarathy, Zhohai Lu, Oscar de Frutos, Pablo A. García
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(10)
During the course of our research efforts to develop potent and selective AKT inhibitors, we discovered enatiomerically pure substituted dihydropyridopyrimidinones (DHP) as potent inhibitors of protein kinase B/AKT with excellent selectivity against
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::107b14709d1a2c2930c8a82be7b68c7d
https://pubmed.ncbi.nlm.nih.gov/29655979
https://pubmed.ncbi.nlm.nih.gov/29655979
Autor:
Kenneth C, Cassidy, Ivelina, Gueorguieva, Colin, Miles, Jessica, Rehmel, Ping, Yi, William J, Ehlhardt
Publikováno v:
Xenobiotica; the fate of foreign compounds in biological systems. 48(4)
1. The disposition and metabolism of galunisertib (LY2157299 monohydrate, a TGF-βRI Kinase/ALK5 Inhibitor) was characterized following a single oral dose of 150 mg of [
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::9a05045bc943cbcc4b896b0027c6dfb0
https://pubmed.ncbi.nlm.nih.gov/29405089
https://pubmed.ncbi.nlm.nih.gov/29405089
Autor:
William J. Ehlhardt, Hao Sun, Garold S. Yost, Christopher A. Reilly, Diane L. Lanza, Palaniappan Kulanthaivel
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 322:843-851
Indoline derivatives possess therapeutic potential within a variety of drug candidates. In this study, we found that indoline is aromatized by cytochrome P450 (P450) enzymes to produce indole through a novel dehydrogenation pathway. The indole produc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be1a5e23fc096e6c6fec1db5e1613ef5
https://doi.org/10.1124/jpet.107.121723
https://doi.org/10.1124/jpet.107.121723
Autor:
Robert D Dally, Yu-Hua Hui, Haitao Hu, Palaniappan Kulanthaivel, Naijia Huang, Ping Yi, William J. Ehlhardt
1. Nuclear magnetic resonance (NMR), a non-selective and inherently quantitative method, has not been widely used as a quantitative tool for characterizing the disposition of lead molecules prior to clinical development. As a test case, we have chose
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e380f43d749f9a44fedf7d479033f9d
Autor:
Palaniappan Kulanthaivel, Jamie L. Renbarger, Robert J. Barbuch, William J. Ehlhardt, Jennifer B. Dennison, Stephen D. Hall
Publikováno v:
Drug Metabolism and Disposition. 34:1317-1327
Clinical outcomes of vincristine therapy, both neurotoxicity and efficacy, are unpredictable, and the reported pharmacokinetics of vincristine have considerable interindividual variability. In vitro and in vivo data support a dominant role for CYP3A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b03064c60b868f6e57998df3712591f
https://doi.org/10.1124/dmd.106.009902
https://doi.org/10.1124/dmd.106.009902
Autor:
Richard M. Schultz, William J. Ehlhardt, John F. Worzalla, Jesse R. Bewley, John E. Toth, Kim K. Klingerman, James Edward Ray, George B. Boder, Gerald B. Grindey, Sharon M. Rinzel, Susan B. Gates, Leonard C. Weir
Publikováno v:
Journal of Medicinal Chemistry. 40:1018-1025
A series of sulfonimidamide analogs of the oncolytic diarylsulfonylureas was synthesized and evaluated for (1) in vitro cytotoxicity against CEM cells, (2) in vivo antitumor activity against subaxillary implanted 6C3HED lymphosarcoma, and (3) metabol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::42671dd536c1464ed18e57726972f7e1
https://doi.org/10.1021/jm960673l
https://doi.org/10.1021/jm960673l
Autor:
William J. Ehlhardt, John M. Mastro, Vinod F. Patel, Julie N. Hardin, James J. Starling, Kevin L. Law, Zimmermann John Lyle, Joseph M. Woodland
Publikováno v:
Bioconjugate Chemistry. 7:497-510
LY207702 (1) is a difluorinated purine nucleoside that exhibits impressive antitumor activity in preclinical models. This agent, however, also possesses cardiotoxicity which limits the potential cl...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c056d6da6e0abf05555d895510515f0f
https://doi.org/10.1021/bc960038u
https://doi.org/10.1021/bc960038u
Autor:
William J. Ehlhardt, Jesse R. Bewley, John F. Worzalla, Joseph M. Woodland, J. Jeffry Howbert, John E. Toth, Glen C. Todd, Gerald B. Grindey
Publikováno v:
Chemical Research in Toxicology. 5:667-673
The metabolic formation of p-chloroaniline from the oncolytic agent sulofenur [N-(5-indanesulfonyl)-N'-(4-chlorophenyl)urea, LY186641,] and from similar diaryl-substituted sulfonylureas, and its possible relevance to the compound's toxicity, was stud
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02e6b4820a14d0bbfa98749511e5099f
https://doi.org/10.1021/tx00029a012
https://doi.org/10.1021/tx00029a012
Autor:
Palaniappan, Kulanthaivel, Robert J, Barbuch, Rita S, Davidson, Ping, Yi, Gregory A, Rener, Edward L, Mattiuz, Chad E, Hadden, Lawrence A, Goodwin, William J, Ehlhardt
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 32(9)
Phase I oxidative metabolism of nitrogen-containing drug molecules to their corresponding N-oxides is a common occurrence. There are instances where liquid chromatography/tandem mass spectometry techniques are inadequate to distinguish this pathway f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::9e887b1b44310fe6ff04f5c0030b8818
https://pubmed.ncbi.nlm.nih.gov/15319338
https://pubmed.ncbi.nlm.nih.gov/15319338
Autor:
David A. Jackson, David E. Moody, Dennis J. Crouch, Palaniappan Kulanthaivel, Robert Espina, Christopher A. Reilly, William J. Ehlhardt, Garold S. Yost, Abdul Mutlib
Publikováno v:
Chemical research in toxicology. 16(3)
Capsaicin is a common dietary constituent and a popular homeopathic treatment for chronic pain. Exposure to capsaicin has been shown to cause various dose-dependent acute physiological responses including the sensation of burning and pain, respirator
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c568631a017075fd872bbe011de650bd
https://pubmed.ncbi.nlm.nih.gov/12641434
https://pubmed.ncbi.nlm.nih.gov/12641434