Bioorganic and Medicinal Chemistry Letters p. 4614 - 4621 (2017)
Update date:2022-08-05
Topics:
Mathew, Bini
Hobrath, Judith V.
Connelly, Michele C.
Kiplin Guy
Reynolds, Robert C.
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.
View MoreCerametek Materials(ShenZhen)Co., Ltd.
Contact:+86-755-2324.2554
Address:A3-#9, YongChuan Street, Suite 501
Wuhan Benjamin Pharmaceutical Chemical Co.,Ltd
Contact:86-27-52341789
Address:Room 1518 B suite, optical valley time square, No 111 Guanshan Road, Hongshan District,Wuhan,Hubei Province,China.
Contact:86 311 85902108 / 85902109
Address:room 1001-1005 ,huanghe Road ,shijiazhuang ,China
Yingkou Sanzheng New Technology Chemical Industry Co., Ltd.
Contact:+86-417-2927806
Address:yingkou
Zhejiang Kente Chemical Co.,Ltd.
Contact:86-0576-87651912
Address:No.7, Fengxi West Road, Modern Industrial Zone
Doi:10.1016/j.chemphyslip.2016.09.003
(2016)Doi:10.1021/ic062041n
(2007)Doi:10.1039/c2dt12309f
(2012)Doi:10.1016/j.bmcl.2008.09.087
(2008)Doi:10.1021/jm201454n
(2012)Doi:10.1139/v63-247
(1963)