Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Rajasree, Golla"'
Autor:
Paul E. Morin, Haixia Wang, Lawrence J. Kennedy, Stephen P. O'connor, James J. Li, Akbar Nayeem, Vidhyashankar Ramamurthy, Steven Sheriff, Nathan Morgan, Steven J. Walker, Xiang-Yang Ye, Frederick Moulin, Brad D. Maxwell, Thomas Harrity, Jeffrey A. Robl, Stephanie Y. Chen, Timothy W. Harper, Rachel Zebo, Jun Li, Zhenqiu Hong, Shung Wu, Mengmeng Wang, Randolph P. Ponticiello, David A. Gordon, Rajasree Golla, Ramakrishna Seethala, Daniel M. Camac, Joseph R. Taylor, David S. Yoon
[Image: see text] BMS-823778 (2), a 1,2,4-triazolopyridinyl-methanol derived analog, was identified as a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) enzyme (IC(50) = 2.3 nM) with >10,000-fold selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::537bf023154f9aff48423a9bc7df61b2
https://europepmc.org/articles/PMC6295842/
https://europepmc.org/articles/PMC6295842/
Autor:
Steven J. Walker, Vidyhashankar Ramamurthy, Jun Li, Shung Wu, David K. Leahy, John D. Dimarco, Brad D. Maxwell, Daniel M. Camac, Joseph R. Taylor, Akbar Nayeem, Zhiwei Guo, James J. Li, Xiang-Yang Ye, Frederick Moulin, Paul E. Morin, Stepen P O’Connor, Haixia Wang, Jeffrey A. Robl, Rachel Zebo, Mark S. Kirby, Thomas Harrity, Joel C. Barrish, Timothy W. Harper, Lawrence L Kennedy, Rajasree Golla, Atsu Apedo, Bogdan Sleczka, Yi-Xin Li, David S. Yoon, Bin He, Steven Sheriff, Ramakrishna Seethala, Nathan Morgan, Mengmeng Wang, Randolph P. Ponticiello, Raymond P. Scaringe, Stephanie Y. Chen, Jianqing Li, Zhenqiu Hong, Ronald L. Hanson, David A. Gordon
Publikováno v:
Journal of medicinal chemistry. 60(12)
BMS-816336 (6n-2), a hydroxy-substituted adamantyl acetamide, has been identified as a novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC50 3.0 nM) with >10000-fold selectivity over human 11β-hydrox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d86602b708c78e42f5648acb482b306b
https://pubmed.ncbi.nlm.nih.gov/28537398
https://pubmed.ncbi.nlm.nih.gov/28537398
Autor:
Ramakrishna Seethala, Steven J. Walker, Jun Li, Stephen P. O'connor, Lawrence J. Kennedy, Steven Sheriff, Rachel Zebo, Daniel M. Camac, Paul E. Morin, Jeffrey A. Robl, Joseph R. Taylor, James J. Li, Haixia Wang, Thomas Harrity, David A. Gordon, Akbar Nayeem, Timothy W. Harper, Zhenqiu Hong, Mengmeng Wang, Randolph P. Ponticiello, Rajasree Golla, Nathan Morgan
Publikováno v:
ACS Medicinal Chemistry Letters. 5:803-808
Small alkyl groups and spirocyclic-aromatic rings directly attached to the left side and right side of the 1,2,4-triazolopyridines (TZP), respectively, were found to be potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase-type 1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f50571624276edc8a5db39e2719422c
https://doi.org/10.1021/ml500144h
https://doi.org/10.1021/ml500144h
Autor:
Mengmeng Wang, Akbar Nayeem, Ramakrishna Seethala, Stephanie Y. Chen, Rajasree Golla, Jeffrey A. Robl, Bin He, Yi-Xin Li, Bogdan Sleczka, David A. Gordon, Xiang-Yang Ye, Timothy W. Harper, Mark S. Kirby
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6699-6704
Starting from high throughput screening hit 2-adamantyl acetic acid 3, a series of polycyclic acids have been designed and synthesized as novel, potent, and selective inhibitors of human 11β-HSD-1. Structure-activity relationships of two different r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::722d41a1003cb116de1e23e259a551b2
https://doi.org/10.1016/j.bmcl.2011.09.055
https://doi.org/10.1016/j.bmcl.2011.09.055
Autor:
Haixia Wang, Ramakrishna Seethala, James J. Li, Yi-Xin Li, Lawrence G. Hamann, Tatyana Zvyaga, Rajasree Golla, David A. Gordon, Ligaya M. Simpkins, Jeffrey A. Robl
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4146-4149
A series of pyridyl amide/sulfonamide inhibitors of 11β-HSD-1 were modified to incorporate a novel 1,2,4-triazolopyridine scaffold. Optimization of substituents at the 3 and 8 position of the TZP core, with a special focus on enhancing metabolic sta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc7ab017017babeea19988c2ca0d1eb1
https://doi.org/10.1016/j.bmcl.2011.05.101
https://doi.org/10.1016/j.bmcl.2011.05.101
Autor:
Ningning Liang, Dong Cheng, Mary Ann Pelleymounter, Tasir Shamsul Haque, Ramakrishna Seethala, Zhengping Ma, Michael A. Poss, William R. Ewing, Rajasree Golla, Cooper Christopher B
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5872-5876
We report the synthesis and enzymatic evaluation of potent inhibitors of acetyl-CoA carboxylases (ACCs) containing biphenyl or 3-phenyl pyridine cores. These compounds inhibit both ACC1 and ACC2, or are moderately selective for either enzyme, dependi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b35e6ffded632a96293c5c862ad13735
https://doi.org/10.1016/j.bmcl.2009.08.077
https://doi.org/10.1016/j.bmcl.2009.08.077
Autor:
Stanley R. Krystek, Donald Egan, John S. Sack, Joyce E. Kuhns, Alexandra A. Nirschl, Gary J. Grover, Rajasree Golla, John A. Lupisella, James A. Bryson, John D. Dimarco, Jack Z. Gougoutas, Ligaya M. Simpkins, Aberra Fura, Jacek Ostrowski, Yan Zou, Yi-Xin Li, Robert Zahler, Yongmi An, James C. Sutton, Kevin Kish, Viral Vyas, Lawrence G. Hamann, Ramakrishna Seethala, Paul G. Sleph, Blake C. Beehler
Publikováno v:
Journal of Medicinal Chemistry. 52:2794-2798
A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of imidazolidin-2-ones. The resulting oxazolidin-2-imines are among the most potent SARMs known, with many ana
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48f214c0cc904cf19d8eb4d61464a864
https://doi.org/10.1021/jm801583j
https://doi.org/10.1021/jm801583j
Autor:
Rajasree Golla, Zhengping Ma, David A. Gordon, Haixia Wang, Yuval Blat, Shung C. Wu, Bhavana Sahni-Arya, Mary Ellen K. Salyan, Donna L. Pedicord, Michael J. Flynn, James J. Li, Cynthia Gates, Laurie Bergeron, Ramakrishna Seethala, Lawrence G. Hamann, Akbar Nayeem
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1774:1184-1191
11beta-hydroxysteroid dehydrogenase 1 regulates the tissue availability of cortisol by interconverting cortisone and cortisol. It is capable of functioning as both a reductase and a dehydrogenase depending upon the surrounding milieu. In this work, w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58bb08318c69c1f2205a7f3a897b8b66
https://doi.org/10.1016/j.bbapap.2007.07.005
https://doi.org/10.1016/j.bbapap.2007.07.005
Autor:
Blake C. Beehler, Gary J. Grover, Alexandra A. Nirschl, Yingzhi Bi, Paul G. Sleph, Mark C. Manfredi, Lawrence G. Hamann, Jacek Ostrowski, Rajasree Golla, Ramakrishna Seethala, James C. Sutton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4487-4490
Replacement of the 3-oxo group of 2-chloro-4-[(7R,7aS)-7-hydroxy-1,3-dioxotetrahydro-1H-pyrrolo[1,2c]imidazol-2(3H)-yl]-3-methylbenzonitrile resulted in a sulfamide series of selective androgen receptor modulator (SARM) agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dda822d6062aa2626d279676e48b537e
https://doi.org/10.1016/j.bmcl.2007.06.007
https://doi.org/10.1016/j.bmcl.2007.06.007
Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications
Autor:
Aberra Fura, James J. Li, Chongqing Sun, Jack Z. Gougoutas, Cindy Y. Li, Gary J. Grover, Viral Vyas, Robert Zahler, Lawrence G. Hamann, Michael Galella, Haixia Wang, Stanley R. Krystek, Alexandra A. Nirschl, Zulan Pi, Rebecca Johnson, Jacek Ostrowski, Blake C. Beehler, Ramakrishna Seethala, Rajasree Golla, James C. Sutton, Yan Zou, Paul G. Sleph
Publikováno v:
Journal of Medicinal Chemistry. 50:3015-3025
A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs), with most of the compounds exhibiting low nM in vitro potency in androgen receptor (AR) bindi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df37f7cee5a90b6fa08090d50ba5a5c7
https://doi.org/10.1021/jm070312d
https://doi.org/10.1021/jm070312d