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Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(α-aminoalkyl)phosphinic acid derivatives against human breast cancer       
Yazarlar
Taner Daştan
Ümit Muhammet Koçyiğit
Cumhuriyet Üniversitesi, Türkiye
Sevgi Durna Daştan
Cumhuriyet Üniversitesi, Türkiye
Pakize Cantürk Kılıçkaya
Cumhuriyet Üniversitesi, Türkiye
Parham Taslimi
Özge Çevik
Adnan Menderes Üniversitesi, Türkiye
Metin Koparır
Fırat Üniversitesi, Türkiye
Öğr. Gör. Dr. Cahit ÖREK Öğr. Gör. Dr. Cahit ÖREK
Kastamonu Üniversitesi, Türkiye
İlhami Gülçin
Atatürk Üniversitesi, Türkiye
Ahmet Çetin
Bingöl Üniversitesi, Türkiye
Özet
The aim of this study was to evaluate biologically active novel molecules having potentials to be drugs by their antitumor properties and by activities of apoptotic caspase and topoisomerase. Following syntheses of novel eight bis(α-aminoalkyl)phosphinic acid derivatives (4a–h) as a result of array of reactions, compounds were evaluated by cytotoxic effects in vitro on human breast cancer (MCF-7) and normal endothelial (HUVEC) cell lines. All phosphinic acid derivatives were effective for cytotoxicity on both MCF-7 and HUVEC lines, while 4c, 4e, and 4f compounds were found significantly more effective. For the evaluation of antitumor properties of compounds in a highly sensitive method, their effects on inhibiting topoisomerases I and II were investigated. Also, some of the bis(α-aminoalkyl)phosphinic acid derivatives (4a, 4e–h) showed nice inhibitory action against acetylcholinesterase and human carbonic anhydrase isoforms I and II.
Anahtar Kelimeler
acetylcholinesterase | carbonic anhydrase | cytotoxicity | phosphinic acid | topoisomerase
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
Dergi ISSN 1095-6670
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q2
Makale Dili İngilizce
Basım Tarihi 11-2017
Cilt No 31
Sayı 11
Sayfalar 21971 / 0
Doi Numarası 10.1002/jbt.21971
Makale Linki http://dx.doi.org/10.1002/jbt.21971