Oxazole and thiazole analogs of sulindac for cancer prevention

Bini Mathew, Judith V. Hobrath, Michele C. Connelly, R. Kiplin Guy, Robert C. Reynolds (Lead / Corresponding author)

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4 Citations (Scopus)
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Abstract

Aim: Experimental and epidemiological studies and clinical trials suggest that nonsteroidal anti-inflammatory drugs possess antitumor potential. Sulindac, a widely used nonsteroidal anti-inflammatory drug, can prevent adenomatous colorectal polyps and colon cancer, especially in patients with familial adenomatous polyposis. Sulindac sulfide amide (SSA) is an amide-linked sulindac sulfide analog that showed in vivo antitumor activity in a human colon tumor xenograft model. Results/methodology: A new analog series with heterocyclic rings such as oxazole or thiazole at the C-2 position of sulindac was prepared and screened against prostate, colon and breast cancer cell lines to probe the effect of these novel substitutions on the activity of sulindac analogs.

Conclusion: In general, replacement of the amide function of SSA analogs had a negative impact on the cell lines tested. A small number of hits incorporating rigid oxazole or thiazole groups in the sulindac scaffold in place of the amide linkage show comparable activity to our lead agent SSA.

Original languageEnglish
Pages (from-to)743-753
Number of pages12
JournalFuture Medicinal Chemistry
Volume10
Issue number7
Early online date19 Apr 2018
DOIs
Publication statusPublished - Apr 2018

Keywords

  • cancer
  • heterocycles
  • NSAIDs
  • oxazole
  • sulindac
  • thiazole

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    Mathew, B., Hobrath, J. V., Connelly, M. C., Guy, R. K., & Reynolds, R. C. (2018). Oxazole and thiazole analogs of sulindac for cancer prevention. Future Medicinal Chemistry, 10(7), 743-753. https://doi.org/10.4155/fmc-2017-0182