Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Dao, Lentz"'
Autor:
Amy Liang, Dao Lentz, Bin Ye, David D. Davey, Karen May, John Parkinson, Beverly King, Hong Ye, Gary Phillips, Robert G. Wei, William J. Guilford, Sabine Schlyer, Lisa M. Mendoza, Selchau Victor, Seock-Kyu Khim, Jih-Lie Tseng, John G. Bauman, Kochanny Monica, Thomas A. Kirkland, Ming Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3891-3894
The synthesis and biological evaluation of a series of N-alkyl glycine amide analogs as LTA(4)-h inhibitors and the importance of the introduction of a benzoic acid group to the potency and pharmacokinetic parameters of our analogs are described. The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56a67c0a4315dcbeaa6a8190f571d4d2
https://doi.org/10.1016/j.bmcl.2008.06.046
https://doi.org/10.1016/j.bmcl.2008.06.046
Autor:
Richard I. Feldman, Gary Phillips, Marc Adler, Daguang Zhu, Elena Ho, Wheeseong Lee, Mark A. Polokoff, Hongyi Yu, Dao Lentz, Marc Whitlow, Arnaiz Damian O, Kochanny Monica, Babu Subramanyam, Imadul Islam, James M. Wu, Judi Bryant, Yuo-Ling Chou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3814-3818
HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca9b5b6c85e996a38c96e34d7d0210bc
https://doi.org/10.1016/j.bmcl.2007.04.071
https://doi.org/10.1016/j.bmcl.2007.04.071
Autor:
Dao Lentz, Marc Whitlow, Kenneth J. Shaw, Karna Lyn Sacchi, Sakata Steven T, Janette Walters, Kathy White, Joseph Post, Bin Ye, Wheeseong Lee, Kochanny Monica, Elena Ho, Amy Liang, Ron Vergona, Janice Ewing, Morrissey Michael M, Karanjawala Rushad E, Gary Phillips, Zuchun Zhao, Brian D. Griedel, Babu Subramanyam, Marc Adler
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:2127-2146
A series of thiophene-containing non-amidine factor Xa inhibitors is described. Simple methyl-substituted thiophene analogs were relatively weak inhibitors. However, introduction of hydrophilic substituents at C-4 or C-5 of the thiophene afforded inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79b4b05420f1f0b4641803f66b53494f
https://doi.org/10.1016/j.bmc.2006.12.019
https://doi.org/10.1016/j.bmc.2006.12.019
Autor:
Dao Lentz, Marc Whitlow, Zheng Chang, Harald Dinter, Mike Ferrer, Silke Finster, Marc Adler, Daguang Zhu, Sandra L. Biroc, Richard I. Feldman, Bruno Alicke, Monica Kochanny, Judi Bryant, Brad O. Buckman, Mark A. Polokoff, Arnaiz Damian O, James M. Wu, Shendong Yuan
Publikováno v:
Journal of Biological Chemistry. 280:19867-19874
The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. Here, we describe three
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5088ddc20f2394f04c36606bd1d432b
https://doi.org/10.1074/jbc.m501367200
https://doi.org/10.1074/jbc.m501367200
Autor:
Kochanny Monica, Dao Lentz, Galina Rumennik, Michael Snider, Joseph Post, David R. Light, John Morser, Amy Liang, Lan Trinh
Publikováno v:
Biochemical Pharmacology. 65:1407-1418
Benzothiophene-anthranilamide 1 (3-chloro- N -[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[ b ]thiophene-2-carboxamide) was discovered by high throughput screening to be a highly potent and selective non-amidine inhibitor of human factor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b765bcaf948d1f3f0fd4ea62f9be6820
https://doi.org/10.1016/s0006-2952(03)00084-4
https://doi.org/10.1016/s0006-2952(03)00084-4
Autor:
Amy Liang, Ron Vergona, Keith Eagen, Janette Walters, David J. Smith, Kenneth J. Shaw, Ng Howard P, Elena Ho, Dao Lentz, Kathy White, Lan Trinh, Babu Subramanyam, Raju Mohan, Gary Phillips, Morrissey Michael M, Mark E. Sullivan, William J. Guilford, Brad O. Buckman, Shung C. Wu, Kochanny Monica
Publikováno v:
Bioorganic & Medicinal Chemistry. 10:657-666
A novel series of triaryloxypyridines have been designed to inhibit factor Xa, a serine protease strategically located in the coagulation cascade. Inhibitor 5e has a K I against factor Xa of 0.12 nM and is greater than 8000- and 2000-fold selective o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::61b28124500c42b131140d9bea08868f
https://doi.org/10.1016/s0968-0896(01)00338-8
https://doi.org/10.1016/s0968-0896(01)00338-8
Autor:
Yuo-Ling Chou, John Morser, Marc Adler, Wheeseong Lee, Joseph Post, David R. Light, Kochanny Monica, Karna Lyn Sacchi, Dao Lentz, Arnaiz Damian O, Marc Whitlow, Bin Ye, Amy Liang, Ron Vergona, Richard W. Fitch, Mark E. Sullivan, Sarah Cheeseman, Janice Ewing, Zuchun Zhao, Babu Subramanyam, Kathy White, Kenneth J. Shaw, Karanjawala Rushad E, Janette Walters, Brian D. Griedel, Yi-Xin Wang, William P. Dole, Michael M. Morrissey, Steven T. Sakata, Galina Rumennik, Shung C. Wu
Publikováno v:
Journal of medicinal chemistry. 50(13)
There remains a high unmet medical need for a safe oral therapy for thrombotic disorders. The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is among the more promising targets for anticoagulant therapy and has bee
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d9b314570fda62e22e2ae9d385e5ac9
https://pubmed.ncbi.nlm.nih.gov/17536795
https://pubmed.ncbi.nlm.nih.gov/17536795
Autor:
Arnaiz Damian O, Judi Bryant, Richard I. Feldman, Mark A. Polokoff, Gary Phillips, Paul Hrvatin, Marc Adler, James M. Wu, Babu Subramanyam, Dao Lentz, Imadul Islam, Marc Whitlow, Daguang Zhu, Kochanny Monica, Jun Shen, Janette Walters, Shendong Yuan, Elena Ho, Greg Brown
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(14)
Based on the lead compound BX-517, a series of C-4' substituted indolinones have been synthesized and evaluated for PDK1 inhibition. Modification at C-4' of the pyrrole afforded potent compounds (7b and 7d) with improved solubility and ADME propertie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69ccd70016040387d3840477d0ee0a34
https://pubmed.ncbi.nlm.nih.gov/17544272
https://pubmed.ncbi.nlm.nih.gov/17544272
Autor:
Amy Liang, Dao Lentz, Lan Trinh, Yuo-Ling Chou, Brad O. Buckman, David R. Light, Raju Mohan, Kenneth J. Shaw, Morrissey Michael M, Meg Mccarrick
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(9)
Reductive amination followed by acylation of polymer-linked formyl aryl amidines generate combinatorial libraries of aryl amidines 8-13. Potent small molecule naphthylamidine inhibitors 12 (Ki
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1d75964e0961f81726be92c98157a24
https://pubmed.ncbi.nlm.nih.gov/15837303
https://pubmed.ncbi.nlm.nih.gov/15837303
Autor:
Bin Ye, Yuo-Ling Chou, Rushad Karanjawala, Wheeseong Lee, Shou-Fu Lu, Kenneth J. Shaw, Steven Jones, Dao Lentz, Amy Liang, Jih-Lie Tseng, Qingyu Wu, Zuchun Zhao
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(3)
Compound 2 was identified by high throughput screening as a novel PAI-1 inhibitor. Systematic optimization of the A, B, and C segments of 2 resulted in the identification of a more potent compound 39 with good oral bioavailability. The synthesis and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8ac8dffc234bb22c20e57c689fb630f
https://pubmed.ncbi.nlm.nih.gov/14741285
https://pubmed.ncbi.nlm.nih.gov/14741285