A small diversity library of α-methyl amide analogs of sulindac for probing anticancer structure-activity relationships

Bini Mathew, Timothy S. Snowden, Michele C. Connelly, R. Kiplin Guy, Robert C. Reynolds

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


Non-steroidal anti-inflammatory drugs (NSAIDs) have a variety of potential indications that include management of pain and inflammation as well as chemoprevention and/or treatment of cancer. Furthermore, a specific form of ibuprofen, dexibuprofen or the S-(+) form, shows interesting neurological activities and has been proposed for the treatment of Alzheimer's disease. In a continuation of our work probing the anticancer activity of small sulindac libraries, we have prepared and screened a small diversity library of α-methyl substituted sulindac amides in the profen class. Several compounds of this series displayed promising activity compared with a lead sulindac analog.

Original languageEnglish
Pages (from-to)2136-2142
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Issue number12
StatePublished - Jul 1 2018

Bibliographical note

Funding Information:
This work was supported by grants from the National Institutes of Health NCI 1R01CA131378 (RCR PI) and DOD Era of Hope award W81XWH-07-1-0463 (RCR PI). We thank Lucile White, Lynn Rasmussen and Melinda Ingram of Southern Research for HTS support services. Additionally, Judith V. Hobrath of the Drug Discovery Unit in the College of Life Sciences at the University of Dundee gave critical input into manuscript preparation and provided information relative to metabolism of the sulindac analogs presented in this work. We would also like to acknowledge contributions by the High Throughput Biology Center in the Department of Chemical Biology and Therapeutics at St. Jude Children’s Research Hospital in Memphis, TN for BJ cell line data and additional anticancer cell line screens. The work at St. Jude was supported by American Lebanese Syrian Associated Charities (ALSAC).

Publisher Copyright:
© 2018 The Authors


  • Anticancer
  • Chemical biology
  • Chemoprevention
  • Profens
  • Sulindac

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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