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 (10)
Taner Dastan Bingöl Üniversitesi, Türkiye
Umit M. Kocyigit Cumhuriyet Üniversitesi, Türkiye
Sevgi Durna Dastan Cumhuriyet Üniversitesi, Türkiye
Pakize Canturk Kilickaya Cumhuriyet Üniversitesi, Türkiye
Doç. Dr. Parham Taslimi Atatürk Üniversitesi, Türkiye
Ozge Cevik Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Metin Koparir Firat Üniversitesi, Türkiye
Öğr. Gör. Dr. Cahit ÖREK Kastamonu Üniversitesi, Türkiye
İlhami Gulçin Atatürk Üniversitesi, Türkiye
Ahmet Cetin Bingöl Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Journal of Biochemical and Molecular Toxicology (Q2)
Dergi ISSN 1095-6670 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 11-2017
Kabul Tarihi Yayınlanma Tarihi 17-08-2017
Cilt / Sayı / Sayfa 31 / 11 / 21971–0 DOI 10.1002/jbt.21971
Makale Linki http://dx.doi.org/10.1002/jbt.21971
UAK Araştırma Alanları
Organik Kimya
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 …
Anahtar Kelimeler
acetylcholinesterase | carbonic anhydrase | cytotoxicity | phosphinic acid | topoisomerase