Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives
   
Yazarlar (8)
Prof. Dr. Meliha Burcu GÜRDERE Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Ali Aydın Yozgat Bozok Üniversitesi, Türkiye
Belkız Yencilek
Fatih Ertürk İstanbul Arel Üniversitesi, Türkiye
Doç. Dr. Oğuz ÖZBEK Zonguldak Bülent Ecevit Üniversitesi
Sultan Erkan Sivas Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Yakup BUDAK Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Makale Türü Açık Erişim Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı CHEMISTRY & BIODIVERSITY (Q4)
Dergi ISSN 1612-1872 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 07-2020
Cilt / Sayı / Sayfa 17 / 7 / – DOI 10.1002/cbdv.202000139
Makale Linki https://onlinelibrary.wiley.com/doi/abs/10.1002/cbdv.202000139
Özet
Novel enamine derivatives were synthesized from the reaction of lactone and chalcones and their antiproliferative and cytotoxic activities against six cancer cell lines (e. g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell lines (e. g., FL) were investigated along with their mode of interactions with CT‐DNA. Most of the enamine derivatives with IC50 values of 86–168 μM demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5‐fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (∼6 nm), indicating that they bind to the DNA by way of an …
Anahtar Kelimeler
antiproliferative activity | chalcone | cytotoxicity, molecular docking | enamine | lactone