Breast cancer (BC), is the most commonly diagnosed cancer and second leading cause of death after lung cancer, among US women. African American women are much more likely to die from it despite the lower incidents. Flavonoids, naturally occurring compounds, are a subject of intensive research as promising anti-cancer agents for various types of malignant growths since they offer a promising and less toxic alternative to the existing treatments. Multiple mechanisms of action have been proposed including enzyme modulation in the pathways leading to cellular growth and proliferation, apoptosis, inflammation, and reversal of multidrug resistance. Most of the research on flavonoids have been focused on polyphenols with different hydroxyl substitution pattern, however our previous experience has proven that other flavonoid derivatives are more potent inhibitors of breast cancer. In this study we report the biological activity of novel synthetic Δ1-pyrroline-5-carbonitriles and flavonoids.Synthetic substituted flavonoids, 2-amino-5-oxonitriles and Δ1-pyrroline-5-carbonitriles with methyl, methoxy, halogen, and hydroxyl groups in the aromatic rings A and B were tested for inhibition of cell growth and proliferation of the following cancer cell lines: Ishikawa, MCF-7, and MDA-MB-231. Some of the chalcone derivatives showed activity comparable to, or superior to tamoxifen and 4-hydroxytamoxifen used as standards with IC50 ranging between 3.57 – 40.66 mM. The same compounds were tested on MBA-MD-231 cell line using taxol, staurosporine, doxorubin, and campothecin as standards where methoxy and methyl substituted Δ1-pyrroline-5-carbonitriles were the most potent agents thus indicating a different mechanism of interaction with the cells. Investigation of the reaction path is in progress.

Inhibition of breast cancer cell growth and proliferation by novel synthetic Δ1-pyrroline-5-carbonitriles and flavonoids

255th National Meeting (2018)

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