Methylpyrrole inhibitors of BET bromodomains

Hasvold, Lisa A.; Sheppard, George S.; Wang, Le; Fidanze, Steven D.; Liu, Dachun; Pratt, John K.; Mantei, Robert A.; Wada, Carol K.; Hubbard, Robbert; Shen, Yu; Lin, Xiaoyu; Huang, Xiaoli; Warder, Scott E.; Wilcox, Denise; Li, Leiming; Buchanan, F. Greg; Smithee, Lauren; Albert, Daniel H.; Magoc, Terrance J.; Park, Chang H.; Petros, Andrew M.; Panchal, Sanjay C.; Sun, Chaohong; Kovar, Peter; Soni, Nirupama B.; Elmore, Steven W.; Kati, Warren M.; McDaniel, Keith F.

doi:10.1016/j.bmcl.2017.02.057

Title: Methylpyrrole inhibitors of BET bromodomains

Journal Article · Mon May 01 00:00:00 EDT 2017 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2017.02.057· OSTI ID:1414004

Hasvold, Lisa A.; Sheppard, George S.; Wang, Le; Fidanze, Steven D.; Liu, Dachun; Pratt, John K.; Mantei, Robert A.; Wada, Carol K.; Hubbard, Robbert; Shen, Yu; Lin, Xiaoyu; Huang, Xiaoli; Warder, Scott E.; Wilcox, Denise; Li, Leiming; Buchanan, F. Greg; Smithee, Lauren; Albert, Daniel H.; Magoc, Terrance J.; Park, Chang H. more »

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Sponsoring Organization:: USDOE

OSTI ID:: 1414004

Journal Information:: Bioorganic and Medicinal Chemistry Letters, Journal Name: Bioorganic and Medicinal Chemistry Letters Vol. 27 Journal Issue: 10; ISSN 0960-894X

Publisher:: ElsevierCopyright Statement

Country of Publication:: United Kingdom

Language:: English

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Cited by: 17 works

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References (18)

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The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition Shi, Junwei; Vakoc, Christopher R. Molecular Cell, Vol. 54, Issue 5 https://doi.org/10.1016/j.molcel.2014.05.016	journal	June 2014
Clinical progress and pharmacology of small molecule bromodomain inhibitors Theodoulou, Natalie H.; Tomkinson, Nicholas CO; Prinjha, Rab K. Current Opinion in Chemical Biology, Vol. 33 https://doi.org/10.1016/j.cbpa.2016.05.028	journal	August 2016
The bromodomain interaction module Filippakopoulos, Panagis; Knapp, Stefan FEBS Letters, Vol. 586, Issue 17 https://doi.org/10.1016/j.febslet.2012.04.045	journal	May 2012
4-Acyl Pyrroles: Mimicking Acetylated Lysines in Histone Code Reading Lucas, Xavier; Wohlwend, Daniel; Hügle, Martin Angewandte Chemie International Edition, Vol. 52, Issue 52 https://doi.org/10.1002/anie.201307652	journal	November 2013
Palladium-catalysed direct arylations of NH-free pyrrole and N-tosylpyrrole with aryl bromides Bheeter, Charles Beromeo; Bera, Jitendra K.; Doucet, Henri Tetrahedron Letters, Vol. 53, Issue 5 https://doi.org/10.1016/j.tetlet.2011.11.081	journal	February 2012
Discovering High-Affinity Ligands for Proteins: SAR by NMR Shuker, S. B.; Hajduk, P. J.; Meadows, R. P. Science, Vol. 274, Issue 5292, p. 1531-1534 https://doi.org/10.1126/science.274.5292.1531	journal	November 1996
Ligand efficiency indices as guideposts for drug discovery Abadzapatero, C.; Metz, J. Drug Discovery Today, Vol. 10, Issue 7 https://doi.org/10.1016/S1359-6446(05)03386-6	journal	April 2005
Genome-wide siRNA screen identifies SMCX, EP400, and Brd4 as E2-dependent regulators of human papillomavirus oncogene expression Smith, Jennifer A.; White, Elizabeth A.; Sowa, Mathew E. Proceedings of the National Academy of Sciences, Vol. 107, Issue 8 https://doi.org/10.1073/pnas.0914818107	journal	February 2010
Structure and ligand of a histone acetyltransferase bromodomain Dhalluin, Christophe; Carlson, Justin E.; Zeng, Lei Nature, Vol. 399, Issue 6735 https://doi.org/10.1038/20974	journal	June 1999
Structure and acetyl-lysine recognition of the bromodomain Mujtaba, S.; Zeng, L.; Zhou, M-M Oncogene, Vol. 26, Issue 37 https://doi.org/10.1038/sj.onc.1210618	journal	August 2007
Targeting bromodomains: epigenetic readers of lysine acetylation Filippakopoulos, Panagis; Knapp, Stefan Nature Reviews Drug Discovery, Vol. 13, Issue 5 https://doi.org/10.1038/nrd4286	journal	April 2014
The chemistry of pyrrolic compounds. XXXVII. Monobenzoporphyrins: The rhodoporphyrin of petroleum deposits Clezy, Ps; Fookes, Cjr; Mirza, Ah Australian Journal of Chemistry, Vol. 30, Issue 6 https://doi.org/10.1071/CH9771337	journal	January 1977
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Suppression of inflammation by a synthetic histone mimic Nicodeme, Edwige; Jeffrey, Kate L.; Schaefer, Uwe Nature, Vol. 468, Issue 7327 https://doi.org/10.1038/nature09589	journal	November 2010

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