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Makale Tam Makale Uluslararası 2017

Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(-aminoalkyl)phosphinic acid derivatives against human breast cancer

Taner Dastan, ÜMİT MUHAMMET KOÇYİĞİT, Sevgi Durna Dastan, Pakize Canturk Kilickaya, Parham TASLIMI, Ozge Cevik, Metin Koparir, Cahit Orek, İlhami Gülçin, Ahmet Cetin

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY Cilt 31 · Sayı 11 · 01.11.2017
DOI ile aç

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(-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(-aminoalkyl)phosphinic acid derivatives (4a, 4e-h) showed nice inhibitory action against acetylcholinesterase and human carbonic anhydrase isoforms I and II.

Anahtar kelimeler

IN-VITRO carbonic anhydrase antioxidant cytotoxicity Pressure Acetylcholinesterase Butyrylcholinesterase Mannich bases ANALOGS BIOACTIVITY BROMOPHENOLS II INHIBITION phosphinic acid topoisomerase

Sürdürülebilir Kalkınma Amaçları

  • SKA 3: Sağlıklı Bireyler

Atıf için künye

Dastan, T., KOÇYİĞİT, Ü. M., Dastan, S. D., Kilickaya, P. C., TASLIMI, P., Cevik, O., Koparir, M., Orek, C., Gülçin, İ., & Cetin, A. (2017). Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(-aminoalkyl)phosphinic acid derivatives against human breast cancer. JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, 31(11). https://doi.org/10.1002/jbt.21971

BibTeX 
@article{dastan2017-67889,
  author = {Dastan, Taner and KOÇYİĞİT, ÜMİT MUHAMMET and Dastan, Sevgi Durna and Kilickaya, Pakize Canturk and TASLIMI, Parham and Cevik, Ozge and Koparir, Metin and Orek, Cahit and Gülçin, İlhami and Cetin, Ahmet},
  title = {Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(-aminoalkyl)phosphinic acid derivatives against human breast cancer},
  journal = {JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY},
  year = {2017},
  volume = {31},
  number = {11},
  issn = {1095-6670},
  doi = {10.1002/jbt.21971},
  url = {https://akademik.atauni.edu.tr/yayinlar/67889-investigation-of-acetylcholinesterase-and-mammalian-dna-topoisomerases-carbonic}
}