The research team was able to design, synthesize and characterize novel chalcone analogs and test them for the potential treatment of invasive breast cancers
Breast cancer is the most commonly reported cancer in females and the leading cause of cancer death in women globally. It is a highly mixed disease with triple negative breast cancer (TNBC) being the most aggressive subtype. TNBCs do not have FDA approved targeted medications yet.
A group of researchers from Qatar University (QU) aimed at the identification and discovery of new alternatives to combat breast cancer. Ms. Dana Elkhalifa (MSc Pharmacy graduate) selected this interesting project as her MSc thesis under the direct supervision of Dr. Ashraf Khalil (Professor of Medicinal Chemistry and Acting Head of Pharmaceutical Sciences Department) and co-supervision of Dr. Ala-Eddin Al Moustafa (Professor of Cell Biology, College of Medicine) and Dr. Feras Alali (Professor and Director of Research and Graduate Studies, QU Health Cluster).
This research project was funded by QU and Qatar National Research Fund (QNRF). The research team was able to design, synthesize and characterize novel chalcone analogs and test them for the potential treatment of invasive breast cancers.
“Chalcone” is a biochemical molecule that is found in a variety of plants including flowers, fruits and vegetables. In literature, it was reported to exert diverse biological activities in different disease conditions like infections, heart diseases, central nervous system disorders and cancer.
Therefore, the team had designed and synthesized 14 novel chalcone analogs bearing different functional groups with potential anticancer activities. They proposed that these molecules could target difficult types of breast cancer like TNBC.
Consequently, the prepared compounds were tested against a panel of TNBC cells in the lab (in vitro). One of these novel molecules was found to be highly effective. It had significantly inhibited cancer cells’ growth, prevented their movement and migration, promoted their physiologic death and had completely inhibited them from forming colonies. It was compared to well establish anticancer medications in the market and found to be superior to them.
Further, the effect of this novel molecule was investigated in animals to test whether it can inhibit new blood vessels formation. Interestingly, there was a 60% inhibition by the novel compound, indicating it can prevent cancer progression. Because these results were very interesting, the research team tested this promising molecule on a mice cancer model (in vivo) injected with invasive breast cancer cells (TNBC). The new molecule was capable of inhibiting cancer cell growth by around 50% as compared to untreated mice.
A US patent was then filed and published (Publication No. US-2020-0392119-A1) on this novel molecule, which is believed to exert a great potential of being developed as an anticancer medication, not only for breast cancer; but hopefully, for other types of cancer.
Currently, the research team is in the process of developing a drug delivery system for this molecule using nanoparticles.
Additionally, they are investigating the anticancer activities of it on other types of breast cancer, namely HER2+, and on colorectal cancer in vitro and in vivo using the Drosophila (small fruit flies) colorectal cancer model.