Abstract
Small molecule DNA intercalators as antineoplastic agents, for breast cancers, have gained a significant amount of success within recent years. Therefore, previously tested naphthalimide compounds were coupled to an estrogen receptor antagonist in offering a useful method in delivering cytotoxic drugs selectively to sites expressing high levels of estrogen receptors. A series of novel conjugate compounds incorporating a linker, with an anhydride component and a diamine component, joining estrogen and known potent naphthalimides were synthesized to demonstrate apoptotic effects with antiproliferative activity in breast cancer cell lines. These conjugates are promising compounds for further studies in treatment of estrogen receptor positive breast cancers. Calculated LD50 values for the antiproliferation assays illustrate a clear structure‐activity relationship for this conjugated naphthalimide‐estrogen series.This abstract is from the Experimental Biology 2018 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.
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