Design, synthesis and biological evaluation of novel bischalcone derivatives as potential anticancer agents
Date
1April 202Author
Burmalıoğlu SerdarGöbek, Arzu
Özturk Aydın,Busra
Yurtoğlu, Emine
Nur Aydın,Busra
Yalcin Ozkat,Gozde
Hepokur, Ceylan
Şimşek Özek, Nihal
Ayşin, Ferhunde
Altundas, Ramazan
Algul,Oztekin
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Show full item recordAbstract
Building on our previous work that discovered chalcone as a promising pharmacophore for anticancer activity,
we have various other chalcone derivatives and have synthesized a series of novel bischalcone to explore their
anticancer activity. Among all tested compounds, compounds 6a, 6b, and 6c showed the highest antiproliferative
activity against A-549 cancer cell lines with the average IC50 values of 4.18, 4.52, and 5.05 µM, respectively.
Moreover, compound 6c showed high antiproliferative activity against the Caco-2 cell line; thus, it was 2- and 4-
fold more active than the reference compounds, i.e., methotrexate and capecitabine. Compound 6a also induced
cell-cycle arrest in the S phase, whereas compounds 6b and 6c were observed to stop at the G0/G1 phase.
Thereafter, we evaluated that compound 6c also had the highest apoptosis/necrosis ratio than other compounds
and the standard compound. The anticancer property of the 6c was also supported by molecular docking studies
carried out on the EGFR and HER2 receptors. Overall, we expect that these compounds can be further developed
for the potential treatment of lung cancer