3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma
Xu, Rui, Wang, Keshi, Rizzi, James P, Huang, Heli, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Wehn, Paul M, Yang, Hanbiao, Dixon, Darryl D, Czerwinski, Robert M, Du, Xinlin, Ged, Emily L, Han, Guangzhou, Tan, Huiling, Wong, Tai, Xie, Shanhai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
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A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma
Wallace, Eli M, Rizzi, James P, Han, Guangzhou, Wehn, Paul M, Cao, Zhaodan, Du, Xinlin, Cheng, Tzuling, Czerwinski, Robert M, Dixon, Darryl D, Goggin, Barry S, Grina, Jonas A, Halfmann, Megan M, Maddie, Melissa A, Olive, Sarah R, Schlachter, Stephen T, Tan, Huiling, Wang, Bin, Wang, Keshi, Xie, Shanhai, Xu, Rui, Yang, Hanbiao, Josey, John A
Published in Cancer research (Chicago, Ill.) (15.09.2016)
Published in Cancer research (Chicago, Ill.) (15.09.2016)
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DNA-dependent protein kinase inhibitors as drug candidates for the treatment of cancer
Kashishian, Adam, Douangpanya, Heather, Clark, Darcey, Schlachter, Stephen T, Eary, C Todd, Schiro, Justin G, Huang, Hongmei, Burgess, Larry E, Kesicki, Edward A, Halbrook, James
Published in Molecular cancer therapeutics (01.12.2003)
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Published in Molecular cancer therapeutics (01.12.2003)
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Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)‑3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro‑1H‑inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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Journal Article
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction
Wehn, Paul M., Yang, Song, Grina, Jonas A., Rizzi, James P., Schlachter, Stephen T., Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Czerwinski, Robert M., Ged, Emily L., Huang, Heli, Halfmann, Megan M., Maddie, Melissa A., Morton, Emily R., Olive, Sarah R., Tan, Huiling, Xie, Shanhai, Josey, John A., Wallace, Eli M.
Published in Medicinal chemistry research (01.07.2023)
Published in Medicinal chemistry research (01.07.2023)
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Discovery of a Novel Class of Imidazo[1,2‑a]Pyridines with Potent PDGFR Activity and Oral Bioavailability
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Published in ACS medicinal chemistry letters (09.01.2014)
Published in ACS medicinal chemistry letters (09.01.2014)
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Carbonyl-Containing Bisphosphonate Esters as Novel Antiinflammatory and Antiarthritic Agents
Nugent, Richard A, Schlachter, Stephen T, Murphy, Megan, Dunn, Colin J, Staite, Nigel D, Galinet, Louise A, Shields, Sharon K, Wu, Haiyan, Aspar, Danielle G, Richard, Karen A
Published in Journal of medicinal chemistry (01.12.1994)
Published in Journal of medicinal chemistry (01.12.1994)
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Pyrimidine Thioethers: A Novel Class of HIV-1 Reverse Transcriptase Inhibitors with Activity Against BHAP-Resistant HIV
Nugent, Richard A, Schlachter, Stephen T, Murphy, Michael J, Cleek, Gary J, Poel, Toni J, Wishka, Donn G, Graber, David R, Yagi, Yoshihiko, Keiser, Barbara J, Olmsted, Robert A, Kopta, Laurie A, Swaney, Steven M, Poppe, Susan M, Morris, Joel, Tarpley, W. Gary, Thomas, Richard C
Published in Journal of medicinal chemistry (24.09.1998)
Published in Journal of medicinal chemistry (24.09.1998)
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Pyrazoline bisphosphonate esters as novel antiinflammatory and antiarthritic agents
Nugent, Richard A., Murphy, Megan, Schlachter, Stephen T., Dunn, Colin J., Smith, Robert J., Staite, Nigel D., Galinet, Louise A., Shields, Sharon K., Aspar, Danielle G., Richard, Karen A., Rohloff, Norman A.
Published in Journal of medicinal chemistry (1993)
Published in Journal of medicinal chemistry (1993)
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ARYL ETHERS AND USES THEREOF
JOSEY JOHN A, DIXON DARRYL DAVID, YANG HANBIAO, GRINA JONAS, SCHLACHTER STEPHEN T, XU RUI, WALLACE ELI M, WEHN PAUL, RIZZI JAMES P, WANG BIN
Year of Publication 17.05.2016
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Year of Publication 17.05.2016
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PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
HENTEMANN MARTIN F, SCHLACHTER STEPHEN T, XIAO DENGMING, LIANG JUN, GRAHAM JAMES M, BLAKE JAMES F, SPENCER KEITH L, BENCSIK JOSEF, MITCHELL IAN S, XU RUI, SAFINA BRIAN S, WELCH MIKE, KALLAN NICHOLAS C
Year of Publication 04.08.2015
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Year of Publication 04.08.2015
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5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES
MORENO DAVID A, SCHLACHTER STEPHEN T, HARVEY DARREN, BOYS MARK LAURENCE, GRONEBERG ROBERT, KRASER CHRISTOPHER F, HACHE BRUNO P, HICKEN ERIK JAMES, ROBINSON JOHN E, REN LI, LAIRD ELLEN, MUNSON MARK C, BURGESS LAURENCE E, EARY C. TODD
Year of Publication 20.06.2014
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Year of Publication 20.06.2014
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HYDROXYLATED AND METHOXYLATED CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS
SCHLACHTER STEPHEN T, XIAO DENGMING, SAFINA BRIAN, BENCSIK JOSEF R, LIANG JUN, BANKA ANNA L, BLAKE JAMES F, MITCHELL IAN S, XU RUI, CHABOT CHRISTINE, ZHANG BIRONG, DO STEVEN, WALLACE ELI M, SPENCER KEITH LEE, KALLAN NICHOLAS C
Year of Publication 11.05.2015
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Year of Publication 11.05.2015
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AKT-PROTEIN KINASE INHIBITOR HYDROXYLATED AND METHOXYLATED CYCLOPENTA [D] PYRIMIDINE
SCHLACHTER STEPHEN T, XIAO DENGMING, SAFINA BRIAN, BENCSIK JOSEF R, LIANG JUN, BANKA ANNA L, BLAKE JAMES F, MITCHELL IAN S, CHABOT CHRISTINE, ZHANG BIRONG, DO STEVEN, SPENCER KEITH LEE, RUI XU, WALLACE ELI W, KALLEN NICHOLAS C
Year of Publication 11.12.2014
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Year of Publication 11.12.2014
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HYDROXYLATED AND METHOXYLATED CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS
SCHLACHTER STEPHEN T, XIAO DENGMING, SAFINA BRIAN, BENCSIK JOSEF R, LIANG JUN, BANKA ANNA L, BLAKE JAMES F, MITCHELL IAN S, XU RUI, CHABOT CHRISTINE, ZHANG BIRONG, DO STEVEN, WALLACE ELI M, SPENCER KEITH LEE, KALLAN NICHOLAS C
Year of Publication 25.07.2014
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Year of Publication 25.07.2014
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HYDROXYLATED AND METHOXYLATED CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS
SCHLACHTER STEPHEN T, XIAO DENGMING, SAFINA BRIAN, BENCSIK JOSEF R, LIANG JUN, BANKA ANNA L, BLAKE JAMES F, MITCHELL IAN S, XU RUI, CHABOT CHRISTINE, ZHANG BIRONG, DO STEVEN, WALLACE ELI M, SPENCER KEITH LEE, KALLAN NICHOLAS C
Year of Publication 26.12.2013
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Year of Publication 26.12.2013
Patent
Abstract B140: PT2977, a novel HIF-2a antagonist, has potent antitumor activity and remodels the immunosuppressive tumor microenvironment in clear cell renal cell cancer
Wong, Tai W., Shrimali, Rajeev, Contreras, Cristina, Cheng, Tzuling, Czerwinski, Robert M., Dixon, Daryl D., Du, Xinlin, Fett, Craig, Goree, Jessica, Grina, Jonas A., Han, Guangzhou, Huang, Heli, Rizzi, Jim, Schlachter, Stephen T., Wang, Bin, Wang, Keshi, Wehn, Paul M., Xie, Shanhai, Xu, Rui, Yang, Hanbiao, Josey, John A., Wallace, Eli M.
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Journal Article
HYDROXYLATED AND METHOXYLATED CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS
SCHLACHTER STEPHEN T, XIAO DENGMING, SAFINA BRIAN, BENCSIK JOSEF R, LIANG JUN, BANKA ANNA L, BLAKE JAMES F, MITCHELL IAN S, XU RUI, CHABOT CHRISTINE, ZHANG BIRONG, DO STEVEN, WALLACE ELI M, SPENCER KEITH LEE, KALLAN NICHOLAS C
Year of Publication 22.03.2013
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Year of Publication 22.03.2013
Patent
PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
HENTEMANN MARTIN F, SCHLACHTER STEPHEN T, XIAO DENGMING, LIANG JUN, GRAHAM JAMES M, BLAKE JAMES F, SPENCER KEITH L, BENCSIK JOSEF, MITCHELL IAN S, XU RUI, SAFINA BRIAN S, WELCH MIKE, KALLAN NICHOLAS C
Year of Publication 30.04.2010
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Year of Publication 30.04.2010
Patent