Cytotoxic effects, carbonic anhydrase isoenzymes, α-glycosidase and acetylcholinesterase inhibitory properties, and molecular docking studies of heteroatom-containing sulfonyl hydrazone derivatives

Hasan Ufuk Celebioglu, Yavuz Erden, Fatma Hamurcu*, Parham Taslimi, Ozan Sanlı Şentürk, Ümmühan Özdemir Özmen, Burak Tuzun, İlhami Gulçin

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)

Abstract

Today, interest in studies on the search for new drugs to be used in diseases such as cancer, cardiovascular diseases, neurodegenerative diseases and diabetes, as well as prevention of microbial inflammation is increasing day by day. Emerging biological and pharmacological effects of sulfonyl hydrazone derivative compounds reveal their importance. In the present study, heteroatom-containing sulfonyl hydrazone derivatives have been studied for their anticancer and antimicrobial properties, as well as their effects on enzymes that could play roles in Alzheimer's dissease and diabetes. High doses of the tested compounds significantly decreased the cell viabilities of breast cancer (MCF-7) and prostate cancer (PC-3) cell lines. Furthermore, all compounds possessed antimicrobial activities against very common bacteria E. coli and S. aureus. These compounds were good inhibitors of the α-glycosidase, human carbonic anhydrase I and II isoforms and acetylcholinesterase enzyme with Ki values in the range of 1.14 ± 0.14–3.63 ± 0.26 nM for α-glycosidase, 66.05 ± 9.21–125.45 ± 11.54 nM for hCA I, 89.14 ± 10.43–170.22 ± 26.05 nM for hCA II and 754.03 ± 73.22–943.92 ± 58.15 nM for AChE, respectively. Molecular docking method was used to theoretically compare biological activities of sulfonyl hydrazone derivatives against enzymes. The theoretical results were compared with the experimental results. Thus, these compounds have strong biological activities. Communicated by Ramaswamy H. Sarma.

Original languageEnglish
Pages (from-to)1-12
Number of pages12
JournalJournal of Biomolecular Structure and Dynamics
DOIs
Publication statusPublished - 2020

Bibliographical note

Publisher Copyright:
© 2020, © 2020 Informa UK Limited, trading as Taylor & Francis Group.

Keywords

  • Heteroatom
  • antibacterial
  • anticancer
  • docking
  • enzyme inhibition
  • sulfonyl hydrazone

Fingerprint

Dive into the research topics of 'Cytotoxic effects, carbonic anhydrase isoenzymes, α-glycosidase and acetylcholinesterase inhibitory properties, and molecular docking studies of heteroatom-containing sulfonyl hydrazone derivatives'. Together they form a unique fingerprint.

Cite this