Diverse amide analogs of sulindac for cancer treatment and prevention
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.
Mathew, Bini,Hobrath, Judith V.,Connelly, Michele C.,Kiplin Guy,Reynolds, Robert C.
supporting information
p. 4614 - 4621
(2017/09/29)
DERIVATIVES OF SULINDAC, USE THEREOF AND PREPARATION THEREOF
Derivatives of sulindac are provided along with-pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.
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Page/Page column 22-23
(2008/06/13)
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