Synthesis and biological evaluation of a cyclic ether fluorinated noscapine analog |
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Authors: | Aneja Ritu Vangapandu Surya N Joshi Harish C |
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Affiliation: | aLaboratory for Drug Discovery and Research, Department of Cell Biology, Emory University School of Medicine, 615 Michael Street, Atlanta, GA 30322, USA |
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Abstract: | We present here a novel semi-synthetic cyclic ether fluorinated noscapine analog (CEFNA) that shows potent antiproliferative and anticancer activity in both hormone-responsive (MCF-7) and hormone non-responsive (MDA-MB-231) breast cancer cells. Interestingly, it is also effective against MCF-7/Adr, an adriamycin-resistant variant of MCF-7 cells. Immunofluorescence experiments showed numerous micronuclei, indicative of apoptotic cell death triggered by this novel analog. Mechanistically, CEFNA exerts a strong antimitotic effect as revealed by cell-cycle studies that show a dose-dependent increase in G2/M population preceding a rising sub-G1 population, suggesting apoptosis. |
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Keywords: | Noscapine Fluorination Cyclic ethers Anticancer |
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