Synthesis, molecular docking, and antitumoral activity of alnustone-like compounds against estrogen receptor alpha-positive human breast cancer

Authors : Kaan Küçükoğlu, Hatice Seçinti, Aykut Özgür, Hasan Seçen, Yusuf Tutar

Pages : 179-193

Doi:10.3906/kim-1408-72

View : 29 | Download : 6

Publication Date : 9999-12-31

Article Type : Makaleler

Abstract :Alnustone-like compounds are promising inhibitors for estrogen receptor a (ER-a), which is a novel cancer therapeutic target. Therefore, 10 alnustone-like compounds with substituents at the phenyl rings were synthesized by condensation of 4-phenyl-2-butanones and cinnamaldehydes via in situ enamination. The compounds displayed either protective activity or inhibited cell growth and proliferation of human breast cancer cells. Molecular docking studies indicated that the synthesized compounds interact with ER-a efficiently. In this work, the protective and inhibitive roles of the synthesized compounds were related to their functional groups and to their binding mode of action on ER-a protein. The compounds are potential drug candidates as ER-a antagonists.
Keywords : Alnustone-like compounds, MCF-7, breast cancer, estrogen receptor a, diarylheptanoids