Journal
BIOCONJUGATE CHEMISTRY
Volume 23, Issue 4, Pages 785-795Publisher
AMER CHEMICAL SOC
DOI: 10.1021/bc200645n
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Funding
- Northeastern University
- Department of Defense [W81XWH-10-1-0262]
- Department of Energy [DE-SC0001781]
- Komen Foundation [BCTR0600659]
- Public Health Service (NIH) [1R01CA121838]
- U.S. Department of Energy (DOE) [DE-SC0001781] Funding Source: U.S. Department of Energy (DOE)
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As part of our program to develop breast cancer specific therapeutic agents, we have synthesized a conjugate agent that is a conjugate of the steroidal anti-estrogen and the potent cytotoxin doxorubicin. In this effort, we employed a modular assembly approach to prepare a novel 11 beta-substituted steroidal anti-estrogen functionalized with an azido-tetraethylene glycol moiety, which could be coupled to a complementary doxorubicin benzoyl hydrazone functionalized with a propargyl tetraethylene glycol moiety. Huisgen [3 + 2] cycloaddition chemistry gave the final hybrid that was evaluated for selective uptake and cytotoxicity in ER(+)-MCF-7 and ER(-)-MDA-MB-231 breast cancer cell lines. The results demonstrated that the presence of the anti-estrogenic component in the hybrid compound was critical for selectivity and cytotoxicity in ER(+)-MCF-7 human breast cancer cells as the hybrid was similar to 70-fold more potent than doxorubicin in inhibition of cell proliferation and promoting cell death.
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