Premium
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
Author(s) -
Dastan Taner,
Kocyigit Umit M.,
Durna Dastan Sevgi,
Canturk Kilickaya Pakize,
Taslimi Parham,
Cevik Ozge,
Koparir Metin,
Orek Cahit,
Gulçin İlhami,
Cetin Ahmet
Publication year - 2017
Publication title -
journal of biochemical and molecular toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.526
H-Index - 58
eISSN - 1099-0461
pISSN - 1095-6670
DOI - 10.1002/jbt.21971
Subject(s) - topoisomerase , chemistry , carbonic anhydrase , cytotoxicity , cytotoxic t cell , in vitro , biochemistry , carbonic anhydrase ii , enzyme , acetylcholinesterase , stereochemistry , apoptosis , cancer cell , cancer , biology , genetics
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.