Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Hovis M. Imade"'
Autor:
Hovis M. Imade, Jiahong Wang, Russell A. Judge, Steven Fung, Martin Winn, Peer B. Jacobson, Bryan K. Sorensen, William J. Chiou, DeAnne Stolarik, Michael E. Brune, Ernst U. Frevert, Wenying Qin, Kenton L. Longenecker, Katina Monzon, J.T. Link, Linda E. Chovan, Jeff Rohde, Xiaoqing Deng, Qi Shuai, Heidi S. Camp, Liping Pan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:527-532
Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd16ecfb427678217cb834cd46ff6f7a
https://doi.org/10.1016/j.bmcl.2006.10.008
https://doi.org/10.1016/j.bmcl.2006.10.008
Autor:
Hovis M. Imade, Hing L. Sham, Liping Pan, Linda E. Chovan, Heidi S. Camp, Bryan K. Sorensen, Rodger F. Henry, Jiahong Wang, Atul Ramaiya, Mark M. Mullally, Rohde Jeffrey J, J.T. Link, William J. Chiou, Katina Monzon, Peer B. Jacobson, Thomas A. Fey, Kennan C. Marsh, Xiaoqing Deng, David W A Beno, DeAnne Stolarik, Brian A. Droz, Steven Fung, Michael E. Brune, Ernst U. Frevert, Marina A. Pliushchev, Qi Shuai, Dariusz Wodka
Publikováno v:
Journal of Medicinal Chemistry. 50:149-164
Starting from a rapidly metabolized adamantane 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor 22a, a series of E-5-hydroxy-2-adamantamine inhibitors, exemplified by 22d and (+/-)-22f, was discovered. Many of these compounds are po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::740a7e4962595eb2ab50d7cba96e3da2
https://doi.org/10.1021/jm0609364
https://doi.org/10.1021/jm0609364
Autor:
Jiahong Wang, DeAnne Stolarik, Hovis M. Imade, Victoria Knourek-Segel, Phong Nguyen, Denise Wilcox, Peer B. Jacobson, Michael E. Brune, William Chiou, Steven Fung, Robin Shapiro, Vince Yeh, J.T. Link, Ravi Kurukulasuriya, Katina Monzon, Eugene N. Bush
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5555-5560
A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16d60418fa06ac90a6a4054cde3829be
https://doi.org/10.1016/j.bmcl.2006.08.034
https://doi.org/10.1016/j.bmcl.2006.08.034
Autor:
William J. Chiou, Jiahong Wang, Jyoti R. Patel, Peer B. Jacobson, Michael E. Brune, J.T. Link, Ravi Kurukulasuriya, Hong Yong, Hing L. Sham, Steven Fung, Katina Monzon, DeAnne Stolarik, Hovis M. Imade, David W A Beno, Vince Yeh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5414-5419
A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::401f7c072da604f9bdd8ef80c7fb5c64
https://doi.org/10.1016/j.bmcl.2006.07.055
https://doi.org/10.1016/j.bmcl.2006.07.055
Autor:
Shi-Chung Ng, Gerard M. Sullivan, Weibo Wang, Hovis M. Imade, Stephen J. O'connor, Haiying Zhang, Hing L. Sham, Stephen L. Gwaltney, Saul H. Rosenberg, Lisa A. Hasvold, Jerome Cohen, Wen-Zhen Gu, Joy Bauch, Qun Li, Stephen K. Tahir, Steve Muchmore, Charles W. Hutchins, Kennan C. Marsh, Nelson Lissa T, Clarissa G. Jakob, Vincent S. Stoll, David Frost
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1359-1362
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bace2fe027ea17136753c78626be974f
https://doi.org/10.1016/s0960-894x(03)00095-7
https://doi.org/10.1016/s0960-894x(03)00095-7
Autor:
Kenneth J. Barr, Hovis M. Imade, Robert B. Warner, David Frost, Stephen L. Gwaltney, Jang Yun Lee, Hing L. Vernon Hills Sham, R. Bruce Credo, Peter Kovar, Jieyi Wang, Laura Gehrke, Qun Li, Nicolette A. Zielinski, Shi Chung Ng, Michael A. Nukkala
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:871-874
Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Import
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6d2f5d2d512fac2dd2b467a6f39dc468
https://doi.org/10.1016/s0960-894x(01)00098-1
https://doi.org/10.1016/s0960-894x(01)00098-1
Autor:
Hovis M. Imade, Stephen L. Gwaltney, Peter Kovar, Shi-Chung Ng, Qun Li, Robert B. Warner, Jang Yun Lee, R. Bruce Credo, Laura Gehrke, David Frost, Hing L. Sham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1671-1673
The synthesis and biological evaluation of novel sulfonate analogues of E-7010 are reported. Several of the compounds are potent inhibitors of cell proliferation and tubulin polymerization. Importantly, these compounds are also active against P-glyco
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ebbdf22522200a39ff06649d45c6d52
https://doi.org/10.1016/s0960-894x(01)00279-7
https://doi.org/10.1016/s0960-894x(01)00279-7
Autor:
David W A Beno, Wenying Qin, J.T. Link, Jiahong Wang, Liping Pan, M. Winn, Peer B. Jacobson, Francis A. J. Kerdesky, Seble Wagaw, Michael E. Brune, Hing L. Sham, Jyoti R. Patel, Russell A. Judge, DeAnne Stolarik, Linda E. Chovan, Jürgen Dinges, Steven Fung, Hovis M. Imade, Qi Shuai, Kenton L. Longenecker, Kenneth M. Engstrom, Katina Monzon, Marina A. Pliushchev, William J. Chiou
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(3)
A novel class of adamantane ethers 11beta-hydroxysteroid hydrogenase type I inhibitors has been discovered. These compounds have excellent HSD-1 potency and selectivity against HSD-2. The structure-activity relationships, selectivity, metabolism, PK,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23500077cfb0881349bea95c319e6699
https://pubmed.ncbi.nlm.nih.gov/17110106
https://pubmed.ncbi.nlm.nih.gov/17110106
Autor:
Charles W. Hutchins, Kennan C. Marsh, Stephen L. Gwaltney, Jerome Cohen, Vincent S. Stoll, Lisa A. Hasvold, Joy Bauch, Steve Muchmore, Gerard M. Sullivan, Qun Li, Weibo Wang, David Frost, Wen-Zhen Gu, Nelson Lissa T, Shi-Chung Ng, Stephen J. O'connor, Stephen K. Tahir, Clarissa G. Jakob, Hovis M. Imade, Saul H. Rosenberg, Haiying Zhang, Hing L. Sham
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(7)
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered bio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2160014edb580afacf5017815d5b8a01
https://pubmed.ncbi.nlm.nih.gov/12657283
https://pubmed.ncbi.nlm.nih.gov/12657283
Autor:
Jeffrey J. Rohde, Marina A. Pliushchev, Bryan K. Sorensen, Dariusz Wodka, Qi Shuai, Jiahong Wang, Steven Fung, Katina M. Monzon, William J. Chiou, Liping Pan, Xiaoqing Deng, Linda E. Chovan, Atul Ramaiya, Mark Mullally, Rodger F. Henry, DeAnne F. Stolarik, Hovis M. Imade, Kennan C. Marsh, David W. A. Beno, Thomas A. Fey
Publikováno v:
Journal of Medicinal Chemistry; Jan2007, Vol. 50 Issue 1, p149-164, 16p