Scopus
YÖKSİS Eşleşti
New indole-7-aldehyde derivatives as melatonin analogues; synthesis and screening their antioxidant and anticancer potential
Bioorganic Chemistry · Kasım 2020
YÖKSİS Kayıtları
New indole-7-aldehyde derivatives as melatonin analogues; synthesis and screening their antioxidant and anticancer potential
BIOORGANIC CHEMISTRY · 2020 SCI-Expanded
DOÇENT HANİF ŞİRİNZADE →
Makale Bilgileri
DergiBioorganic Chemistry
Yayın TarihiKasım 2020
Cilt / Sayfa104
Scopus ID2-s2.0-85090353710
Özet
Over the last decade, there has been substantial interest in the use of melatonin (MLT) and MLT-like compounds in the treatment of several diseases. MLT can scavenge different reactive oxygen species and can also stimulate the synthesis of antioxidant enzymes. Our ongoing study relies on changing the groups in the different modifiable sites of the indole ring to increase the antioxidant activity. In this study a new approach for substitution of indole ring as indole based MLT analogue was proposed. We report the synthesis and characterization of a series of new indole-7-aldehyde hydrazide/hydrazone derivatives as indole-based MLT analogues. Anticancer potential of the compounds were evaluated both by their antioxidant and CYP1 inhibitory activities. In vitro antioxidant capacity of the compounds was investigated both in a cell-based (DCFH assay) and a cell-free (DPPH assay) assay. Potential inhibitory effects of the compounds on CYP1 catalytic activity were investigated via EROD assay. Cytotoxic activity of the compounds was further evaluated by the MTT assay in CHO-K1 cells. MLT analogues having an o-halogenated aromatic moiety exhibited effective antioxidant properties without having any cytotoxic effect. In conclusion, MLT derivatives represent promising scaffolds for discovery of effective antioxidant agents.
Yazarlar (6)
1
Hanif Şirinzade
2
Eddy Neuhaus
3
Elif Ince Erguc
4
Alev Tascioglu Aliyev
5
Hande Gurer-Orhan
6
Sibel Süzen
Anahtar Kelimeler
Antioxidant activity
CYP1 inhibition
Cytotoxicity
Indole
Melatonin
Synthesis
Kurumlar
Ankara Üniversitesi
Ankara Turkey
Ege Üniversitesi
Izmir Turkey
Erzincan Binali Yıldırım Üniversitesi
Erzincan Turkey
İzmir Kâtip Çelebi Üniversitesi
Izmir Turkey
Metrikler
17
Atıf
6
Yazar
6
Anahtar Kelime