- Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines
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A small library of emetine dithiocarbamate ester derivatives were synthesized in 25-86% yield via derivatization of the N2′- position of emetine. Anticancer evaluation of these compounds in androgen receptor positive LNCaP and androgen receptor negative P
- Akinboye, Emmanuel S.,Bamji, Zebalda D.,Kwabi-Addo, Bernard,Ejeh, David,Copeland, Robert L.,Denmeade, Samuel R.,Bakare, Oladapo
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p. 5839 - 5845
(2015/11/11)
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- EMETINE DERIVATIVES, PRODRUGS CONTAINING SAME, AND METHODS OF TREATING CONDITIONS USING SAME
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Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2'-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.
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Page/Page column 20-23
(2012/12/13)
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