Synthesis, molecular docking, and antitumoral activity of alnustone-like compounds against estrogen receptor alpha-positive human breast cancer      
Yazarlar (5)
Kaan Küç Üko Glu
Atatürk Üniversitesi, Türkiye
Hatice Seç Inti
Atatürk Üniversitesi, Türkiye
Doç. Dr. Aykut ÖZGÜR Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Hasan Seçen
Atatürk Üniversitesi, Türkiye
Yusuf Tutar
Cumhuriyet Üniversitesi, Türkiye
Makale Türü Açık Erişim Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Turkish Journal of Chemistry
Dergi ISSN 1300-0527 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q4
Makale Dili İngilizce
Basım Tarihi 01-2015
Cilt No 39
Sayı 1
Sayfalar 179 / 193
DOI Numarası 10.3906/kim-1408-72
Makale Linki https://dctubitak.researchcommons.org/chem/vol39/iss1/17/
Özet
Abstract: Alnustone-like compounds are promising inhibitors for estrogen receptor \alpha (ER-\alpha), 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-\alpha 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-\alpha protein. The compounds are potential drug candidates as ER-\alpha antagonists.
Anahtar Kelimeler
Alnustone-like compounds | Breast cancer | Diarylheptanoids | Estrogen receptor α | MCF-7