Heterocyclic Schiff base derivatives containing pyrazolone moiety: Synthesis, characterization, and in vitro biological studies
Yükleniyor...
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Wiley
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
In this study, some pyrazolone-based Schiff base derivatives 2a-e (except 2a)were synthesized for the first time and structurally illuminated by some spec-troscopic techniques (1H,13C NMR, FT-IR) and elemental analysis. Allsynthesized molecules were screened for their anticancer and antioxidantactivities, as well as AChE, BChE, and tyrosinase inhibitory properties.The obtained results exhibited that compounds 1b (IC50= 9.497 Μ) and 2a(IC50= 30.49 Μ) significantly decreased the proliferation of HeLa cells. Onthe other hand, the apoptotic effects of these two compounds were investigatedwith acridine orange/propidium iodide double staining. The apoptotic cellratios of the molecules treated with these two compounds were determined as60 and 64%. Compound 2b (IC50= 17.95 ± 0.47 Μ ) was determined to be avery active substance in the ABTS assay. Compound 2e (A0.5= 43.75± 0.62 M) indicated the closest antioxidant activity to the standard compoundα-TOC (A0.5= 50.58 ± 0.39 M) in the cupric reducing antioxidant capacity(CUPRAC) assay. In inhibition studies of enzymes, it was determined thatcompound 2c had a very active molecule in AChE, BChE, and tyrosinaseinhibitory activities with 82.79 ± 1.03, 91.39 ± 1.06, and 92.60 ± 1.80% inhibi-tion, respectively. It was determined that the target molecules 2a-e showedbetter antioxidant and enzyme inhibitory activities than those of ester deriva-tives 1a-e.
Açıklama
WOS:000709844600001
Anahtar Kelimeler
Anticancer activity, Antioxidant activity, Enzymes inhibitory, Heterocyclic Schiff base
Kaynak
Journal of the Chinese Chemical Society
WoS Q Değeri
Q4
Scopus Q Değeri
Q2
Cilt
68
Sayı
12
Künye
Çınar, E., Başaran, E., Erdoğan, Ö., Çakmak, R., Boğa, M. ve Çevik, Ö. (2021). Heterocyclic Schiff base derivatives containing pyrazolone moiety: Synthesis, characterization, and in vitro biological studies. Journal of the Chinese Chemical Society, Early Access.
