Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Rosanna Tedesco"'
Autor:
Mary Ann Hardwicke, Hong Lin, Karl F. Erhard, John D. Martin, Ren Xie, Kaushik Raha, Rosanna Tedesco, Jin Zeng, Yanqiu Qian, Patricia M. Kratz, Yong Jiang, Ted Cecconie, Stan F. Martens, Angela Smallwood, Patrick McDevitt, James F. Mack, Baoguang Zhao, Stephenie B. Chen, Anthony J. Jurewicz, Juan I. Luengo, Mark J. Schulz, Nino Campobasso, Catherine A. Oleykowski, Lawrence M. Szewczuk, Alan R. Rendina, Cynthia M. Rominger, Benjamin J. Schwartz, Leng Nickels, Junya Qu, Jacques Briand
Publikováno v:
ACS Medicinal Chemistry Letters. 7:217-222
A novel series of potent and selective hexokinase 2 (HK2) inhibitors, 2,6-disubstituted glucosamines, has been identified based on HTS hits, exemplified by compound 1. Inhibitor-bound crystal structures revealed that the HK2 enzyme could adopt an "in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aec5386353626ba6f7f23a2d64607cd6
https://doi.org/10.1021/acsmedchemlett.5b00214
https://doi.org/10.1021/acsmedchemlett.5b00214
Autor:
Nannan Liu, Michael N. Zimmerman, Richard M. Keenan, Victor K. Johnston, Deping Chai, Rosanna Tedesco, Duke M. Fitch, Juili Lin-Goerke, Kenneth Wiggall, Antony N. Shaw, Nestor O. Concha, Ramesh Bambal, Michael G. Darcy, Robert T. Sarisky, Dashyant Dhanak, Kevin J. Duffy, Adam T. Gates
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4350-4353
The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb2ff5c553e8d62c4eb72b3845398b47
https://doi.org/10.1016/j.bmcl.2009.05.091
https://doi.org/10.1016/j.bmcl.2009.05.091
Autor:
Chao Han, Warren W. Gerhardt, Dashyant Dhanak, Kevin J. Duffy, Nestor O. Concha, Adam T. Gates, Richard M. Keenan, Victor K. Johnston, Glenn A. Hofmann, Duke M. Fitch, Nannan Liu, Kenneth Wiggall, Antony N. Shaw, Dina L. Halegoua, Robert T. Sarisky, Michael N. Zimmerman, Ramesh Bambal, Michael G. Darcy, Arun C. Kaura, Juili Lin-Goerke, Deping Chai, Rosanna Tedesco
Publikováno v:
Journal of Medicinal Chemistry. 49:971-983
Recently, we disclosed a new class of HCV polymerase inhibitors discovered through high-throughput screening (HTS) of the GlaxoSmithKline proprietary compound collection. This interesting class of 3-(1,1-dioxo-2H-1,2,4-benzothiadiazin-3-yl)-4-hydroxy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cae20df8f691062dcbdf7b76d9840b9
https://doi.org/10.1021/jm050855s
https://doi.org/10.1021/jm050855s
Autor:
C. Cheng Kao, Tammy T. Nguyen, Dashyant Dhanak, Lester L. Gutshall, Richard R. Gontarek, Rosanna Tedesco, Michael G. Darcy, Baohua Gu, Robert T. Sarisky, Kevin J. Duffy, Victor K. Johnston
Publikováno v:
Journal of Biological Chemistry. 278:16602-16607
The hepatitis C virus (HCV) NS5B protein encodes an RNA-dependent RNA polymerase (RdRp), the primary catalytic enzyme of the HCV replicase complex. Recently, two benzo-1,2,4-thiadiazine compounds were shown to be potent, highly specific inhibitors of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4f0cb22e1674e58d17a46e746ebb9a4
https://doi.org/10.1074/jbc.m210891200
https://doi.org/10.1074/jbc.m210891200
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1281-1284
To prepare novel estrogen receptor (ER) ligands, we have developed a facile approach to substituted hexahydrochrysene and tetrahydrobenzo[ a ]fluorene systems. Substituents, including basic side chains, were added to these systems, and their binding
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8121df25210640161c26acf7ecad6ca
https://doi.org/10.1016/s0960-894x(01)00189-5
https://doi.org/10.1016/s0960-894x(01)00189-5
Publikováno v:
Chemistry & Biology. 8(3):277-287
Background: The specificity of hormone action arises from complementary steric and electronic interactions between a hormonal ligand and its cognate receptor. An analysis of such key ligand–receptor contact sites, often delineated by mutational map
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00e9dda3ce4c0d8c01e022d690edb28b
Autor:
Ying Huang, Rosanna Tedesco, Shaun R. Stauffer, Christopher J Coletta, John A. Katzenellenbogen
Publikováno v:
Bioorganic & Medicinal Chemistry. 9:141-150
Previously, we reported that certain tetrasubstituted 1,3,5-triaryl-4-alkyl-pyrazoles bind to the estrogen receptor (ER) with high affinity (Fink, B. E.; Mortenson, D. S.; Stauffer, S. R.; Aron, Z. D.; Katzenellenbogen, J. A. Chem. Biol. 1999, 6, 205
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c633208d9983b14cd4c024c25eaf4d6
https://doi.org/10.1016/s0968-0896(00)00228-5
https://doi.org/10.1016/s0968-0896(00)00228-5
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2919-2924
To investigate whether the estrogen receptor accommodates 7α and 11β substituents on estradiol in two subsites or in a single subsite, we have prepared three sets of ligands bearing single (7α or 11β) or double (7α and 11β) substituents and mea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::072e4194412a1be2cce0cbb94fc34597
https://doi.org/10.1016/s0960-894x(97)10099-3
https://doi.org/10.1016/s0960-894x(97)10099-3
Publikováno v:
Tetrahedron Letters. 38:7997-8000
6-Ketoestradiol derivatives are converted in 7α-alkyl substituted estradiol derivatives selectively by alkylation of the generated enolate followed by deoxygenation-deprotection with BF3·Et2O/Et3SiH. © 1997 Elsevier Science Ltd.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e2fcb78aa3457e4da73b39f438364f75
https://doi.org/10.1016/s0040-4039(97)10180-0
https://doi.org/10.1016/s0040-4039(97)10180-0
Autor:
Hong Lin, Charles B. Davis, Kaushik Raha, Ralph A. Rivero, Michael D. Schaber, Jeanelle McSurdy-Freed, Mary Ann Hardwicke, Karl F. Erhard, James F. Mack, Ren Xie, Michael D. Spengler, Ramona Plant, Cynthia M. Rominger, Junya Qu, Rosanna Tedesco, Jennifer L. Ariazi, Juan I. Luengo, Mark J. Schulz, Michael D. Squire, Christian S. Sherk, Jin Zeng
A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ace88350b0677b6d5e549d1aab456577
https://europepmc.org/articles/PMC4025772/
https://europepmc.org/articles/PMC4025772/
