Παρασκευή 20 Απριλίου 2018

Oxazole and thiazole analogs of sulindac for cancer prevention.

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Oxazole and thiazole analogs of sulindac for cancer prevention.

Future Med Chem. 2018 Apr 19;:

Authors: Mathew B, Hobrath JV, Connelly MC, Guy RK, Reynolds RC

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.

PMID: 29671617 [PubMed - as supplied by publisher]



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