Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Kenneth J. Leavitt"'
Autor:
Eric S Muise, Hong-Ping Guan, Jinqi Liu, Andrea R Nawrocki, Xiaodong Yang, Chuanlin Wang, Carlos G Rodríguez, Dan Zhou, Judith N Gorski, Marc M Kurtz, Danqing Feng, Kenneth J Leavitt, Lan Wei, Robert R Wilkening, James M Apgar, Shiyao Xu, Ku Lu, Wen Feng, Ying Li, Huaibing He, Stephen F Previs, Xiaolan Shen, Margaret van Heek, Sandra C Souza, Mark J Rosenbach, Tesfaye Biftu, Mark D Erion, David E Kelley, Daniel M Kemp, Robert W Myers, Iyassu K Sebhat
Publikováno v:
PLoS ONE, Vol 14, Iss 2, p e0211568 (2019)
Physical activity promotes metabolic and cardiovascular health benefits that derive in part from the transcriptional responses to exercise that occur within skeletal muscle and other organs. There is interest in discovering a pharmacologic exercise m
Externí odkaz:
https://doaj.org/article/f28b2c263a184739b47d79a0d7b9272a
Autor:
Hong-Ping Guan, Wen Feng, Daniel M. Kemp, Judith N. Gorski, Shiyao Xu, Ying Li, Dan Zhou, Ku Lu, Tesfaye Biftu, David E. Kelley, Chuanlin Wang, Sandra C. Souza, Lan Wei, Danqing Feng, Robert R. Wilkening, Andrea R. Nawrocki, Iyassu K. Sebhat, Mark J. Rosenbach, Margaret van Heek, Carlos G. Rodriguez, Eric S. Muise, Xiaodong Yang, Mark D. Erion, Jinqi Liu, Stephen F. Previs, James M. Apgar, Marc M. Kurtz, Huaibing He, Robert W. Myers, Xiaolan Shen, Kenneth J. Leavitt
Publikováno v:
PLoS ONE, Vol 14, Iss 2, p e0211568 (2019)
PLoS ONE
PLoS ONE
Physical activity promotes metabolic and cardiovascular health benefits that derive in part from the transcriptional responses to exercise that occur within skeletal muscle and other organs. There is interest in discovering a pharmacologic exercise m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e74f669b91225dbd7a81a386f22662b
https://doaj.org/article/f28b2c263a184739b47d79a0d7b9272a
https://doaj.org/article/f28b2c263a184739b47d79a0d7b9272a
Autor:
Hongjian Zhang, Brian E. Fink, David R. Langley, Harold Mastalerz, Ming Chang, Punit Marathe, Simone Oppenheimer, Dolatrai M. Vyas, Ping Chen, Bogdan Sleczka, John S. Tokarski, Francis Y. Lee, Kenneth J. Leavitt, Johnson Walter Lewis, Wen-Ching Han, Tai W. Wong, Ashvinikumar V. Gavai, Guifen Zhang, Henry Wong, Gregory D. Vite, Tarrant James G, Derek J. Norris
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4947-4954
Pyrrolotriazine dual EGFR/HER2 kinase inhibitors with a 5-((4-aminopiperidin-1-yl)methyl) solubilizing group were found to be superior to analogs with previously reported C-5 solubilizing groups. New synthetic methodology was developed for the parall
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::021672493e2ee4914b09e6b283807847
https://doi.org/10.1016/j.bmcl.2007.06.019
https://doi.org/10.1016/j.bmcl.2007.06.019
Autor:
Johnni Gullo-Brown, Michael A. Poss, Wayne Vaccaro, Tram N. Huynh, Stephanie Barbosa, Carolyn S. Ricca, Mark E. Salvati, Veeraswamy Manne, Zhong Chen, Kenneth J. Leavitt, Soong-Hoon Kim, David R. Tortolani, Donna D. Wei
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:628-632
The synthesis and SAR of a series of pyrrolopyridazine MEK inhibitors are reported. Optimal activity was achieved by incorporation of a 4-phenoxyaniline substituent at C4 and an acylated amine at C6.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9b1ce0dc69568349a8c7b57436978aa
https://doi.org/10.1016/j.bmcl.2005.10.052
https://doi.org/10.1016/j.bmcl.2005.10.052
Autor:
Bruce M. Rankin, William J. Pitts, William J. Metzler, Kenneth J. Leavitt, Andrew T. Pudzianowski, Wayne Vaccaro, Richard Liu, Patricia A. McDonnell, Joseph Barbosa, Soong-Hoon Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1101-1106
Computer aided drug design led to a new class of spiro-barbiturates (e.g., 4a, MMP-13 K(i)=4.7 nM) that are potent inhibitors of MMP-13.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb80a697ae0815fd51299759604589da
https://doi.org/10.1016/j.bmcl.2004.12.016
https://doi.org/10.1016/j.bmcl.2004.12.016
Autor:
Bharat P. Patel, Gregory D. Vite, Gregory Scott Martin, Kenneth J. Leavitt, Lana M. Rossiter, Hongjian Zhang, Francis Y. Lee, Chiang Yu, Arvind Mathur, Simone Oppenheimer, Shankar Swaminathan, John S. Tokarski, Ashvinikumar V. Gavai, Derek J. Norris, Christian L. Holst, Tai W. Wong, Punit Marathe, Wen-Ching Han, Dolatrai M. Vyas, Soong-Hoon Kim, David J. Fairfax, Harold Mastalerz, Joseph Fargnoli, Brian E. Fink, Bindu Goyal
Publikováno v:
Journal of medicinal chemistry. 52(21)
Structure-activity relationships in a series of 4-[1H-indazol-5-ylamino]pyrrolo[2,1-f][1,2,4]triazine-6-carbamates identified dual human epidermal growth factor receptor (HER)1/HER2 kinase inhibitors with excellent biochemical potency and kinase sele
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b25d642f72ade19941b80c3a648395cc
https://pubmed.ncbi.nlm.nih.gov/19821562
https://pubmed.ncbi.nlm.nih.gov/19821562
Autor:
Mark E. Salvati, Jonathan Lippy, Brian E. Fink, Linda K. Stadnick, Robert V. Moquin, Soong-Hoon Kim, John S. Tokarski, Matthew V. Lorenzi, Gregory G. Vite, Ping Chen, Dan You, Kenneth J. Leavitt, Mary T. Obermeier, George L. Trainor
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(2)
2-Amino-5-(thioaryl)thiazoles are potent inhibitors of TrkA (e.g., 20h , TrkA IC 50 = 0.6 nM) that show anti-proliferative effect in cellular assays. A proposed inhibitor binding mode to TrkA active site is consistent with key SAR observations.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b15c4b91bfbccc3c0fa591d817fc342e
https://pubmed.ncbi.nlm.nih.gov/18055203
https://pubmed.ncbi.nlm.nih.gov/18055203
Autor:
Steven Mortillo, Donna D. Wei, Daniel W. Kukral, Viral Vyas, Arvind Mathur, Stephanie Barbosa, Laurence I. Wu, John T. Hunt, Zhen-Wei Cai, Soong-Hoon Kim, Robert Jeyaseelan, Kenneth J. Leavitt, Sam T. Chao, Joseph Fargnoli, Joel C. Barrish, Ligang Qian, Amrita Kamath, Punit Marathe, Xiaoping Zheng, Barri Wautlet, Yong-Zheng Zhang, Leslie Leith, Louis J. Lombardo, Celia D’Arienzo, George M. Derbin, Rajeev S. Bhide, Robert M. Borzilleri, Aberra Fura
Publikováno v:
Journal of medicinal chemistry. 49(7)
A series of substituted 4-(4-fluoro-1H-indol-5-yloxy)pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of vascular endothelial growth factor receptor-2 kinase is reported. Structure-activity relationship studies revealed that a methyl group at the 5-pos
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::439b47c951b45c2e8b163b987da049cc
https://pubmed.ncbi.nlm.nih.gov/16570908
https://pubmed.ncbi.nlm.nih.gov/16570908
Autor:
Gregory D. Vite, Kenneth J. Leavitt, John T. Hunt, Toomas Mitt, Soong-Hoon Kim, John F. Kadow, Donald Crews, Harold Mastalerz, Brian E. Fink, Dolatrai M. Vyas, Tai W. Wong, Karen Du, John S. Tokarski
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(21)
A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c4ad91bfb1cead40c46999beed4c2cc
https://pubmed.ncbi.nlm.nih.gov/16111887
https://pubmed.ncbi.nlm.nih.gov/16111887
Autor:
Byron H. Long, Craig R. Fairchild, John D. Dimarco, Francis Y. Lee, Gerhard Höfle, Gregory D. Vite, Jack Z. Gougoutas, Soong-Hoon Kim, Michael Kiffe, Kenneth J. Leavitt, Alicia Regueiro-Ren
Publikováno v:
Organic letters. 4(22)
[formula: see text] 3-Cyano epothilones 15-18 are the only examples of non-hydroxy C-3-substituted analogues. Their tubulin binding affinity and cytotoxicity provide meaningful structure-activity relationship information on the dependence of C-1/C-3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef89c4ca8a74e7c34492551dc8be6b6e
https://pubmed.ncbi.nlm.nih.gov/12599466
https://pubmed.ncbi.nlm.nih.gov/12599466