Zobrazeno 1 - 10
of 71
pro vyhledávání: '"Frank Boschelli"'
Autor:
Manuel Hidalgo, Antonio Jimeno, Fernando Lopez-Rios, Elena Garcia-Garcia, Frank Boschelli, Christina Coughlin, Max Follettie, Sung E. Choe, Veronica Diesl, Xiao Fei Wang, Aik Choon Tan, N.V. Rajeshkumar, Wells A. Messersmith
Supplementary Fig. S3 from Efficacy and pharmacodynamic effects of bosutinib (SKI-606), a Src/Abl inhibitor, in freshly generated human pancreas cancer xenografts
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a283acce3e612fa6b3d8d6502c06853
https://doi.org/10.1158/1535-7163.22485789.v1
https://doi.org/10.1158/1535-7163.22485789.v1
Autor:
Manuel Hidalgo, Antonio Jimeno, Fernando Lopez-Rios, Elena Garcia-Garcia, Frank Boschelli, Christina Coughlin, Max Follettie, Sung E. Choe, Veronica Diesl, Xiao Fei Wang, Aik Choon Tan, N.V. Rajeshkumar, Wells A. Messersmith
Recently, Src tyrosine kinase has emerged as an attractive target for anticancer therapy, and Src is overexpressed in pancreatic cancer. The purpose of the study was to investigate the in vivo efficacy and pharmacodynamic effects of bosutinib (SKI-60
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f19a0ba0db20c46d9c3033ef510a8d2
https://doi.org/10.1158/1535-7163.c.6532080.v1
https://doi.org/10.1158/1535-7163.c.6532080.v1
Autor:
Zhong Li, Judy Lucas, Jonathan D. Bloom, Russell Dushin, Hao Liu, Mercy Otteng, Mark Johnson, Thomas Nittoli, Jeremy I. Levin, Andrea Olland, Jennifer M. Golas, Christoph W. Zapf, Erik Vogan, Antonia A. Nikitenko, Frank Boschelli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4602-4607
An extension of our previously reported series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. Addition of a second methyl group to the tether provided analogs that show increased potency in binding as well as cell-proliferation ass
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::292118865b349b233211d45dbcb33006
https://doi.org/10.1016/j.bmcl.2011.05.102
https://doi.org/10.1016/j.bmcl.2011.05.102
Autor:
Judy Lucas, Russell Dushin, Christoph W. Zapf, Jamie L. McBean, Hao Liu, Jennifer M. Golas, Frank Boschelli, Erik Vogan, Jeremy I. Levin, Jonathan D. Bloom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3627-3631
A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. In continuation of our research, heterocycle-containing tethers were explored with the intent to further improve potency and minimize hERG liabilities. This effort culmi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba4697a421ffa5a6182e3ba0584b4346
https://doi.org/10.1016/j.bmcl.2011.04.102
https://doi.org/10.1016/j.bmcl.2011.04.102
Autor:
Charles Ingalls, Christoph W. Zapf, Hao Liu, Thomas Nittoli, Judy Lucas, Erik Vogan, Jamie L. McBean, Russell Dushin, Mercy Otteng, Jeremy I. Levin, Frank Boschelli, Yongbo Hu, Jennifer M. Golas, Bloom Jonathan David
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3411-3416
A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. In continuation of our research in this area, macrocyclic amides and lactams were explored to reduce the risk of hERG liabilities. This effort culminated in the discover
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56e86ec59ece02b676d71192cfd60f61
https://doi.org/10.1016/j.bmcl.2011.03.112
https://doi.org/10.1016/j.bmcl.2011.03.112
Autor:
Charles Ingalls, Yongbo Hu, Jeremy I. Levin, Jennifer M. Golas, Clark Eid, Jamie L. McBean, Russell Dushin, Hao Liu, Christoph W. Zapf, Erik Vogan, John P. Sonye, Jonathan D. Bloom, Thomas Nittoli, Alan G. Sutherland, Frank Boschelli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2278-2282
A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. A basic nitrogen within the tether linking the aniline nitrogen atom to a tetrahydroindolone moiety allowed access to compounds with good physical properties. Important
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cabfd0f4263ef6a43713db09d489049c
https://doi.org/10.1016/j.bmcl.2011.02.101
https://doi.org/10.1016/j.bmcl.2011.02.101
Autor:
Frank Boschelli, Judy Lucas, Daniel Wang, Erick Honores, Inder Chaudhary, Diane H. Boschelli, Jennifer M. Golas, Yan Wang, Biqi Wu, Ana Carolina Barrios Sosa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2924-2927
The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC50 values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1f894ee0202ec1e293be393b3575b38
https://doi.org/10.1016/j.bmcl.2010.03.025
https://doi.org/10.1016/j.bmcl.2010.03.025
Autor:
Elena García-García, Aik Choon Tan, Christina Marie Coughlin, N. V. Rajeshkumar, Xiaofei Wang, Sung E. Choe, Antonio Jimeno, Max Follettie, Wells A. Messersmith, Fernando López-Ríos, Veronica Diesl, Manuel Hidalgo, Frank Boschelli
Publikováno v:
Molecular Cancer Therapeutics. 8:1484-1493
Recently, Src tyrosine kinase has emerged as an attractive target for anticancer therapy, and Src is overexpressed in pancreatic cancer. The purpose of the study was to investigate the in vivo efficacy and pharmacodynamic effects of bosutinib (SKI-60
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ce7416cafb1a9671d7d0d5da2198aea
https://doi.org/10.1158/1535-7163.mct-09-0075
https://doi.org/10.1158/1535-7163.mct-09-0075
Autor:
Vera Magistroni, Luca Mologni, Rocco Piazza, Loredana Cleris, Carlo Gambacorti-Passerini, Frank Boschelli, Franca Formelli
Publikováno v:
International Journal of Cancer. 124:1990-1996
Unbalanced histone deacetylase (HDAC) hyperactivity is a common feature of tumor cells. Inhibition of HDAC activity is often associated with cancer cell growth impairment and death. Valproic acid (VPA) is a HDAC inhibitor used for the treatment of ep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1703fa8d85e85aeed8a11b0806023b81
https://doi.org/10.1002/ijc.24158
https://doi.org/10.1002/ijc.24158
Autor:
Myka Estes, Ann H. Williams, Yukiyasu Ozawa, Frank Boschelli, Alan F. List, Richard Jove, Norimasa Matsushita
Publikováno v:
Leukemia Research. 32:893-903
We investigated the role of Src family kinases (SFKs) in the regulation of STAT activation in myeloid leukemia cells. Two of 6 AML cell lines displayed constitutive STAT5 activation, whereas four cell lines had constitutive SFK activity. Treatment wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6277abf5e9b7be2be4aee3ad3c772d2
https://doi.org/10.1016/j.leukres.2007.11.032
https://doi.org/10.1016/j.leukres.2007.11.032