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Items: 11

1.

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 R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD, Czerwinski RM, Du X, Ged EL, Han G, Tan H, Wong T, Xie S, Josey JA, Wallace EM.

J Med Chem. 2019 Aug 8;62(15):6876-6893. doi: 10.1021/acs.jmedchem.9b00719. Epub 2019 Jul 8.

PMID:
31282155
2.

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 PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM.

J Med Chem. 2018 Nov 8;61(21):9691-9721. doi: 10.1021/acs.jmedchem.8b01196. Epub 2018 Oct 18.

PMID:
30289716
3.

A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.

Wallace EM, Rizzi JP, Han G, Wehn PM, Cao Z, Du X, Cheng T, Czerwinski RM, Dixon DD, Goggin BS, Grina JA, Halfmann MM, Maddie MA, Olive SR, Schlachter ST, Tan H, Wang B, Wang K, Xie S, Xu R, Yang H, Josey JA.

Cancer Res. 2016 Sep 15;76(18):5491-500. doi: 10.1158/0008-5472.CAN-16-0473. Epub 2016 Sep 6.

4.

Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Hicken EJ, Marmsater FP, Munson MC, Schlachter ST, Robinson JE, Allen S, Burgess LE, DeLisle RK, Rizzi JP, Topalov GT, Zhao Q, Hicks JM, Kallan NC, Tarlton E, Allen A, Callejo M, Cox A, Rana S, Klopfenstein N, Woessner R, Lyssikatos JP.

ACS Med Chem Lett. 2013 Nov 12;5(1):78-83. doi: 10.1021/ml4003953. eCollection 2014 Jan 9.

5.

DNA-dependent protein kinase inhibitors as drug candidates for the treatment of cancer.

Kashishian A, Douangpanya H, Clark D, Schlachter ST, Eary CT, Schiro JG, Huang H, Burgess LE, Kesicki EA, Halbrook J.

Mol Cancer Ther. 2003 Dec;2(12):1257-64.

6.

Anti-inflammatory/antiarthritic ketonic bisphosphonic acid esters.

Schlachter ST, Galinet LA, Shields SK, Aspar DG, Dunn CJ, Staite ND, Nugent RA.

Bioorg Med Chem Lett. 1998 May 5;8(9):1093-6.

PMID:
9871714
7.

Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV.

Nugent RA, Schlachter ST, Murphy MJ, Cleek GJ, Poel TJ, Wishka DG, Graber DR, Yagi Y, Keiser BJ, Olmsted RA, Kopta LA, Swaney SM, Poppe SM, Morris J, Tarpley WG, Thomas RC.

J Med Chem. 1998 Sep 24;41(20):3793-803.

PMID:
9748354
8.

(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.

Wishka DG, Graber DR, Kopta LA, Olmsted RA, Friis JM, Hosley JD, Adams WJ, Seest EP, Castle TM, Dolak LA, Keiser BJ, Yagi Y, Jeganathan A, Schlachter ST, Murphy MJ, Cleek GJ, Nugent RA, Poppe SM, Swaney SM, Han F, Watt W, White WL, Poel TJ, Thomas RC, Morris J, et al.

J Med Chem. 1998 Apr 23;41(9):1357-60. No abstract available.

PMID:
9554867
9.

Carbonyl-containing bisphosphonate esters as novel antiinflammatory and antiarthritic agents.

Nugent RA, Schlachter ST, Murphy M, Dunn CJ, Staite ND, Galinet LA, Shields SK, Wu H, Aspar DG, Richard KA.

J Med Chem. 1994 Dec 23;37(26):4449-54.

PMID:
7818726
10.

Demonstration of novel anti-arthritic and anti-inflammatory effects of diphosphonates.

Dunn CJ, Galinet LA, Wu H, Nugent RA, Schlachter ST, Staite ND, Aspar DG, Elliott GA, Essani NA, Rohloff NA, et al.

J Pharmacol Exp Ther. 1993 Sep;266(3):1691-8.

PMID:
8371167
11.

Pyrazoline bisphosphonate esters as novel antiinflammatory and antiarthritic agents.

Nugent RA, Murphy M, Schlachter ST, Dunn CJ, Smith RJ, Staite ND, Galinet LA, Shields SK, Aspar DG, Richard KA, et al.

J Med Chem. 1993 Jan 8;36(1):134-9.

PMID:
8421279

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