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 language | English |
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Pages (from-to) | 743-753 |
Number of pages | 11 |
Journal | Future Medicinal Chemistry |
Volume | 10 |
Issue number | 7 |
DOIs | |
State | Published - Apr 2018 |
Bibliographical note
Publisher Copyright:© 2018 2018 Robert C Reynolds.
Keywords
- NSAIDs
- cancer
- heterocycles
- oxazole
- sulindac
- thiazole
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology
- Drug Discovery