Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Joseph Thomas Repine"'
Autor:
John Quin, Peter L. Toogood, Ellen Myra Dobrusin, R. John Booth, William Elliott, Scott Norman Vanderwel, Patricia J. Harvey, Joseph Thomas Repine, Paul R. Keller, David W. Fry, Dennis Joseph Mcnamara
Publikováno v:
Journal of Medicinal Chemistry. 48:2371-2387
Inhibition of the cell cycle kinase, cyclin-dependent kinase-4 (Cdk4), is expected to provide an effective method for the treatment of proliferative diseases such as cancer. The pyrido[2,3-d]pyrimidin-7-one template has been identified previously as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::785108d4129bffdf26a0331ec8e989da
https://doi.org/10.1021/jm049355+
https://doi.org/10.1021/jm049355+
Autor:
Kathleen M. Welch, Joan A. Keiser, M. A. Flynn, Aurash Shahripour, Mark Stephen Plummer, Chet Lee, Billy R. Reisdorph, Ron Rubin, Brian Tobias, Jeremy J. Edmunds, Kent A. Berryman, Hussein Hallak, Annette Marian Doherty, S. J. Haleen, E. E. Reynolds, Joseph Thomas Repine, William C. Patt
Publikováno v:
Journal of Medicinal Chemistry. 40:1063-1074
The design of potent and selective non-peptide antagonists of endothelin-1 (ET-1) and its related isopeptides are important tools defining the role of ET in human diseases. In this report we will describe the detailed structure-activity relationship
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90a850ffc7dc579c406b79be3cc10fea
https://doi.org/10.1021/jm9606507
https://doi.org/10.1021/jm9606507
Autor:
Eric L. Reyner, Hussein Hallak, S. J. Haleen, Joseph Thomas Repine, Kathleen M. Welch, Donnelle M. Walker, Billy R. Reisdorph, M. A. Flynn, Annette Marian Doherty, Barbra H. Stewart, William C. Patt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:297-302
Continued SAR around our ETA selective series of butenolide antagonists, for example PD156707 (1) has yielded a new series of subnanomolar ETA selective antagonists. Depending upon solution pH, 1 exists as the ring closed butenolide form (shown) or a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6a707f757d0c095ca543c68da435d75e
https://doi.org/10.1016/s0960-894x(97)00002-4
https://doi.org/10.1016/s0960-894x(97)00002-4
Autor:
Christine Humblet, Elizabeth A. Lunney, Gerhard Wagner, Joseph Thomas Repine, Venkataraman Thanabal, Michael D. Reily
Publikováno v:
FEBS Letters. 302:97-103
A macrocyclic renin inhibitor was designed using molecular modeling and a model of human renin. The synthesized molecule displayed poor binding affinity. To investigate the reasons for the observed inactivity, the structure of the compound has been s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a621878cc41d35dc8855634715e6e14
https://doi.org/10.1016/0014-5793(92)80293-p
https://doi.org/10.1016/0014-5793(92)80293-p
Autor:
William C. Patt, Bill R. Reisdorph, S. J. Haleen, Annette Marian Doherty, Mark A. Massa, Joseph Thomas Repine, Chet Lee, Richard L. Schroeder, M. A. Flynn, John W. Bryant, Joan A. Keiser, Donnelle M. Walker, Kathleen M. Welch, Xue-Min Cheng
Publikováno v:
Journal of medicinal chemistry. 42(12)
Continued development around our ETA-selective endothelin (ET) antagonist 1 (CI-1020) has led to the synthesis of analogues with improved aqueous solubility profiles. Poor solubility characteristics displayed by 1 required a complex buffered formulat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::092447179b77713e07997510faf64188
https://pubmed.ncbi.nlm.nih.gov/10377221
https://pubmed.ncbi.nlm.nih.gov/10377221
Autor:
Stephen T. Rapundalo, James Stanley Kaltenbronn, Richard Himmelsbach, Joseph Thomas Repine, Christine Humblet, James Marino Hamby, Brian Edward Kornberg, Elizabeth A. Lunney, A M Doherty, Taylor
Publikováno v:
Journal of medicinal chemistry. 35(6)
A series of renin inhibitors having alpha-heteroatom amino acids as P2 substitutions has been prepared. Examples where the heteroatom is oxygen, sulfur, or nitrogen are described. Many of the compounds exhibit subnanomolar potency when tested in vitr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1831a30d535e0eb00c4ab219da19aed
https://pubmed.ncbi.nlm.nih.gov/1552498
https://pubmed.ncbi.nlm.nih.gov/1552498
Autor:
Elizabeth A. Lunney, Christine Humblet, Tom L. Blundell, Joseph Thomas Repine, Jonathan B. Cooper, Bancinyane Lynn Sibanda
Publikováno v:
Advances in Experimental Medicine and Biology ISBN: 9781468460148
In the absence of an accurate three-dimensional structure of human renin, the crystal structures of fungal enzymes have provided reasonable templates for the elaboration of a renin model.1 In addition, the increasing number of bound inhibitor structu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::daa8237273497f80442001cc9be31cd6
https://doi.org/10.1007/978-1-4684-6012-4_51
https://doi.org/10.1007/978-1-4684-6012-4_51
