Title:Evaluation of Fourteen Aurone Derivatives as Potential Anti-Cancer Agents
VOLUME: 18 ISSUE: 5
Author(s):Gheda Alsaif, Nadin Almosnid, Ian Hawkins, Zachary Taylor, Deborah L.T. Knott, Scott Handy, Elliot Altman and Ying Gao*
Affiliation:Department of Biology, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132, , Department of Biology, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132, , Department of Chemistry, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132,, Department of Chemistry, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132,, Tennessee Center for Botanical Medicine Research, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132, Department of Chemistry, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132,, Department of Biology, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132,, Department of Biology, Middle Tennessee State University, 1301 East Main St, Murfreesboro, TN 37132
Keywords:Aurones, benzofuranone, anti-cancer, selectivity, apoptosis, cell motility.
Abstract:Background: Aurones are a sub-set of the flavone family that possess a number of biological
activities, including anti-cancer, anti-inflammatory, anti-microbial, anti-parasitic and anti-viral. Due
to their high availability, simple synthesis, and generally low toxicity, aurones could be attractive candidates
for safer cancer drugs. This study aims to evaluate the anti-proliferation and anti-metastasis activity
of a series of synthesized aurone derivatives.
Methods: A series of aurone derivatives with simple unsubstituted coumaranone (benzofuranone)
fragments and a range of alkylidene fragments have been prepared and tested for anti-proliferation activity
against human cancer cell lines A549 (lung), BT20 (breast) and MCF7 (breast), and antimetastasis
activity against A549.
Results: Several of these compounds displayed significant levels of activity and high levels of selectivity
for the inhibition of the growth of cancerous cell lines versus the corresponding normal cell lines.
This growth inhibition was found to be associated with the induction of apoptosis in cancer cells.
Moreover, several aurone derivatives showed remarkable inhibition on the motility of lung cancer cells
A549 at a concentration as low as 6.25 μM. Analysis of the structure-activity relationship revealed that
the aurone derivatives based upon five-membered heteroaromatic rings exhibited the most significant
anti-cancer activity.
Conclusion: Aurone derivatives devoid of the unusual oxygenation found in the coumaranone fragment
are potential leads for new anti-cancer agents.
