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Diverse Amide Analogs of Sulindac for Cancer Treatment and Prevention

Diverse Amide Analogs of Sulindac for Cancer Treatment and Prevention

Bini Mathew, Judith V Hobrath, Michele C Connelly, R Kiplin Guy, Robert C Reynolds

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4614-4621.

PMID: 28935266

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP53933601	Sulindac Related Compound A		53933-60-1	Price

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