Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Somarajan J. Nair"'
Autor:
Christian M. Martin, Jennifer Proctor, Patrick O'Hearn, Janid A. Ali, Andre Lescarbeau, Jennifer Hoyt, Jonathan P. DiNitto, Ann M. Rowley, Thomas T. Tibbitts, Catherine A. Evans, Martin R. Tremblay, Tao Liu, Vito J. Palombella, John Soglia, Johan A. Pradeilles, Somarajan J. Nair, Melissa Pink, David G. Winkler, Stanley Goldstein, Quentin Glenadel, Erin L. O’Hearn, Culver Cheung, Erin Brophy, Alfredo C. Castro, Louis Grenier
Publikováno v:
ACS Medicinal Chemistry Letters. 7:862-867
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10f2e63c8dbb32a50d02e0a4d22c2564
https://doi.org/10.1021/acsmedchemlett.6b00238
https://doi.org/10.1021/acsmedchemlett.6b00238
Autor:
Michael Foley, Andre Lescarbeau, Martin R. Tremblay, Lombardy Richard John, Grogan Michael John, Andrew B. Hague, Kristopher M. Depew, Jimin Xiong, Joseph Helble, Priscilla L. White, Julian Adams, Brian C. Austad, Caroline D. Lory, Somarajan J. Nair, Stéphane Peluso, Lin-Chen Yu, Alfredo C. Castro, André B. Charette, Benjamin S. Lane, Jeanne Shaffer, Louis Grenier, James R. Porter, Matthew Campbell, Koney Nii O, Mark L. Behnke
Publikováno v:
Organic Process Research & Development. 20:786-798
The formation of the d-homocyclopamine ring system in IPI-926 is the key step in its semisynthesis and proceeds via a chemoselective cyclopropanation followed by a stereoselective acid-catalyzed carbocation rearrangement. In order to perform large-sc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4a9debb0b604cbda59d104def86c7642
https://doi.org/10.1021/acs.oprd.6b00048
https://doi.org/10.1021/acs.oprd.6b00048
Autor:
Martin Trudeau, Louis Grenier, Kristopher M. Depew, Daniel G. Genov, Alexandre Côté, Brian C. Austad, Lin-Chen Yu, Andre Lescarbeau, Theodore A. Martinot, Priscilla L. White, Joseph Helble, Somarajan J. Nair
Publikováno v:
Organic Process Research & Development. 19:1693-1702
A design of experiments (DoE) approach was taken to optimize purity and reaction yield of the final debenzylation and hydrochloride salt formation of IPI-926. The study involved a careful dissection of the different process steps to enable an indepen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::303b6bb1bcb0f53d2408fcb4957573f0
https://doi.org/10.1021/acs.oprd.5b00214
https://doi.org/10.1021/acs.oprd.5b00214
Autor:
Joi Dunbar, Margaret A. Read, Joseph D. Manna, Alexander Constan, Alfredo C. Castro, Sherri Smith, Gordon Loewen, John Lee, Somarajan J. Nair, Jennifer Hoyt, Martin R. Tremblay, Julian Adams, Jeanne A. Ferguson, Jens Sydor, Veronica Campbell, Matthew Campbell, Karen McGovern, Brendan Arsenault, Marisa O. Peluso, Jylle Nevejans, Vito J. Palombella, Nigel Whitebread, Grogan Michael John, Kerrie Faia, John Soglia, Bennett Carter
Publikováno v:
Xenobiotica. 43:875-885
1. IPI-926 is a novel semisynthetic cyclopamine derivative that is a potent and selective Smoothened inhibitor that blocks the hedgehog signal transduction pathway. 2. The in vivo clearance of IPI-926 is low in mouse and dog and moderate in monkey. T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50620a2c18fbef25785c49cf6a0c9deb
https://doi.org/10.3109/00498254.2013.780671
https://doi.org/10.3109/00498254.2013.780671
Autor:
Patrick O'Hearn, Janid A. Ali, Kelly Slocum, Jitendra D. Belani, Sherri Smith, Tao Liu, Adilah Bahadoor, Andre Lescarbeau, Somarajan J. Nair, Christian C. Fritz, Karen McGovern, Kip A. West, Joseph Helble, Bonnie Tillotson, Martin R. Tremblay, Wylie Andrew A, Vito J. Palombella, Alfredo C. Castro, Stéphane Peluso, James M. Conley, Mark Douglas
Publikováno v:
Journal of Medicinal Chemistry. 55:8859-8878
Misregulation of protein translation plays a critical role in human cancer pathogenesis at many levels. Silvestrol, a cyclopenta[b]benzofuran natural product, blocks translation at the initiation step by interfering with assembly of the eIF4F transla
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca8e686d0a86b9c6d0b9d6e0f79d708d
https://doi.org/10.1021/jm3011542
https://doi.org/10.1021/jm3011542
Autor:
Matthew Campbell, Caroline N. Woodward, Jens Sydor, Alfredo C. Castro, James R. Porter, Margaret A. Read, Kerrie Faia, Kerry White, Martin R. Tremblay, Jill Cushing, Julian Adams, Lin-Chen Yu, Mark L. Behnke, Jennifer Hoyt, Vito J. Palombella, Karen McGovern, Somarajan J. Nair, Jeffrey K. Tong, Margit Hagel, Marta Nevalainen, Louis Grenier, Michael Foley
Publikováno v:
Journal of Medicinal Chemistry. 51:6646-6649
Herein is reported the synthesis of a novel class of hedgehog antagonists derived from cyclopamine. The acid sensitive D-ring of cyclopamine was homologated utilizing a sequence of chemoselective cyclopropanation and stereoselective acid-catalyzed re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0d0752adc424ed0f2bb4f871b70a4f4
https://doi.org/10.1021/jm8008508
https://doi.org/10.1021/jm8008508
Autor:
Andre Lescarbeau, Jennifer L. Proctor, Vivian Villegas, Christian M. Martin, Catherine A. Evans, Matthew Rausch, Jeffery L. Kutok, Katherine H. Walsh, Martin R. Tremblay, Janid A. Ali, Jeremy H. Tchaicha, Karen McGovern, Stanley Goldstein, Nicole Kosmider, Vito J. Palombella, Tao Liu, Somarajan J. Nair, Melissa Pink, Alfredo C. Castro, Kerrie Faia, John Soglia, Kerry White, Jonathan P. DiNitto, Erin Brophy, David W. Winkler, Sujata Sharma
Publikováno v:
Cancer Immunology Research. 4:B029-B029
Introduction: The phosphoinositide-3-kinase (PI3K) lipid kinases are a family of kinase isoforms that transduce signals in response to various stimuli in different cell types. The PI3K-γ isoform is expressed in immune cells and has limited, if any,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e973e61c210deebf5b68346ffca26e95
https://doi.org/10.1158/2326-6074.cricimteatiaacr15-b029
https://doi.org/10.1158/2326-6074.cricimteatiaacr15-b029
Autor:
Matthew Campbell, Eddy Tan, Kerry White, Vito J. Palombella, Julian Adams, James M. Conley, Jennifer Hoyt, Martin R. Tremblay, Margit Hagel, Jens Sydor, Jeanne A. Ferguson, Jill Cushing, Alfredo C. Castro, Somarajan J. Nair, Andre Lescarbeau, Melissa Pink, Joseph D. Manna, Grogan Michael John, Margaret A. Read, Caroline N. Woodward, Grace Lin, Mark L. Behnke, Teresa M. Alvarez-Diez, Michael Curtis, Lin-Chen Yu, John R. MacDougall, Karen McGovern, Brian C. Austad
Publikováno v:
Journal of medicinal chemistry. 52(14)
Recent evidence suggests that blocking aberrant hedgehog pathway signaling may be a promising therapeutic strategy for the treatment of several types of cancer. Cyclopamine, a plant Veratrum alkaloid, is a natural product antagonist of the hedgehog p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2605d8d446344a594f8572549b6a22f4
https://pubmed.ncbi.nlm.nih.gov/19522463
https://pubmed.ncbi.nlm.nih.gov/19522463
Autor:
Martin R. Tremblay, André Lescarbeau, Michael J. Grogan, Eddy Tan, Grace Lin, Brian C. Austad, Lin-Chen Yu, Mark L. Behnke, Somarajan J. Nair, Margit Hagel, Kerry White, James Conley, Joseph D. Manna, Teresa M. Alvarez-Diez, Jennifer Hoyt, Caroline N. Woodward, Jens R. Sydor, Melissa Pink, John MacDougall, Matthew J. Campbell
Publikováno v:
Journal of Medicinal Chemistry; Jul2009, Vol. 52 Issue 14, p4400-4418, 19p
Autor:
Martin R. Tremblay, Marta Nevalainen, Somarajan J. Nair, James R. Porter, Alfredo C. Castro, Mark L. Behnke, Lin-Chen Yu, Margit Hagel, Kerry White, Kerrie Faia, Louis Grenier, Matthew J. Campbell, Jill Cushing, Caroline N. Woodward, Jennifer Hoyt, Michael A. Foley, Margaret A. Read, Jens R. Sydor, Jeffrey K. Tong, Vito J. Palombella
Publikováno v:
Journal of Medicinal Chemistry; Oct2008, Vol. 51 Issue 21, p6646-6649, 4p