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- W2043938659 abstract "This study explores the possible use of reactive oxygen-activated DNA modifying agents against acute myeloid leukemia (AML). A key amine on the lead agent was investigated via cytotoxicity assays and was found necessary for potency. The two best compounds were screened via the NCI-60 cell panel. These two compounds had potency between 200 and 800 nM against many of the leukemia cancer cell types. Subsequent experiments explored activity against a transformed AML model that mimics the molecular signatures identified in primary AML patient samples. A lead compound had an IC50 of 760 nM against this AML cell line as well as a therapeutic index of 7.7 ± 3 between the transformed AML model cell line and non-cancerous human CD34+ blood stem/progenitor cells (UCB). The selectivity was much greater than the mainstays of AML treatment: doxorubicin and cytarabine. This manuscript demonstrates that this novel type of agent may be useful against AML." @default.
- W2043938659 created "2016-06-24" @default.
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- W2043938659 date "2013-05-01" @default.
- W2043938659 modified "2023-09-27" @default.
- W2043938659 title "Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia" @default.
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- W2043938659 doi "https://doi.org/10.1016/j.bmcl.2013.03.048" @default.
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