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Optimization of ether and aniline based inhibitors of lactate dehydrogenase

  1. Author:
    Christov, Plamen P.
    Kim, Kwangho
    Jana, Somnath
    Romaine, Ian M.
    Rai, Ganesha
    Mott, Bryan T.
    Allweil, Alexander A.
    Lamers, Alexander
    Brimacombe, Kyle R.
    Urban, Daniel J.
    Lee, Tobie D.
    Hu, Xin
    Lukacs, Christine M.
    Davies, Douglas R.
    Jadhav, Ajit
    Hall, Matthew D.
    Green, Neal
    Moore,Bill
    Stott,Gordon
    Flint,Andrew
    Maloney, David J.
    Sulikowski, Gary A.
    Waterson, Alex G.

  2. Author Address

    Vanderbilt Univ, Vanderbilt Inst Chem Biol, Nashville, TN 37232 USA.Natl Ctr Adv Translat Sci, NIH, 9800 Med Ctr Dr, Rockville, MD 20850 USA.Beryllium Discovery Corp, 7869 Day Rd West, Bainbridge Isl, WA 98110 USA.Leidos Biomed Res Inc, NExT Program Support, Frederick Natl Lab Canc Res, Appl Dev Res Directorate, Frederick, MD 21702 USA.
    1. Year: 2021
    2. Date: Jun 1
    3. Epub Date: 2021 Mar 24
  2. Journal: Bioorganic & Medicinal Chemistry Letters
  3. Pergamon-Elsevier Science Ltd
    1. 41
    2. Pages: 127974
  5. Type of Article: Article
  6. Article Number: ARTN 127974
  7. ISSN: 0960-894X
  1. Abstract:

    Lactate dehydrogenase (LDH) is a critical enzyme in the glycolytic metabolism pathway that is used by many tumor cells. Inhibitors of LDH may be expected to inhibit the metabolic processes in cancer cells and thus selectively delay or inhibit growth in transformed versus normal cells. We have previously disclosed a pyrazolebased series of potent LDH inhibitors with long residence times on the enzyme. Here, we report the elaboration of a new subseries of LDH inhibitors based on those leads. These new compounds potently inhibit both LDHA and LDHB enzymes, and inhibit lactate production in cancer cell lines.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2021.127974
  3. PMID: 33771585
  4. PMCID: PMC8113097
  5. View record in Web of Science®
  6. WOS: 000647660700009

Library Notes

  1. Fiscal Year: FY2020-2021
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