Kaan KÜÇÜKOĞLU, Hatice SEÇİNTİ, Aykut ÖZGÜR, Hasan SEÇEN, Yusuf TUTAR

116108

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

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.
Anahtar Kelimeler:

Alnustone-like compounds, MCF-7, breast cancer, estrogen receptor a, diarylheptanoids

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

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,

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  • Statistical analysis
  • Differences in the mean values of the measured activities were evaluated statistically using SPSS 17.0 (univariate variance analyses and Pearson correlation). Probability values of P < 0.05 were considered significant. 4. Conclusions
Turkish Journal of Chemistry-Cover
  • ISSN: 1300-0527
  • Yayın Aralığı: 6
  • Yayıncı: TÜBİTAK
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