Diverse amide analogs of sulindac for cancer treatment and prevention

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

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)
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Abstract

Sulindac is a non-steroidal anti-inflammatory drug (NSAID) that has shown significant anticancer activity. Sulindac sulfide amide (1) possessing greatly reduced COX-related inhibition relative to sulindac displayed in vivo antitumor activity that was comparable to sulindac in a human colon tumor xenograft model. Inspired by these observations, a panel of diverse sulindac amide derivatives have been synthesized and their activity probed against three cancer cell lines (prostate, colon and breast). A neutral analog, compound 79 was identified with comparable potency relative to lead 1 and activity against a panel of lymphoblastic leukemia cell lines. Several new series also show good activity relative to the parent (1), including five analogs that also possess nanomolar inhibitory potencies against acute lymphoblastic leukemia cells. Several new analogs identified may serve as anticancer lead candidates for further development.

Original languageEnglish
Pages (from-to)4614-4621
Number of pages8
JournalBioorganic & Medicinal Chemistry Letters
Volume27
Issue number20
Early online date13 Sep 2017
DOIs
Publication statusPublished - 15 Oct 2017

Keywords

  • NSAIDs
  • Sulindac
  • Amides
  • Cancer

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