TY - JOUR
T1 - Cytotoxic effects, carbonic anhydrase isoenzymes, α-glycosidase and acetylcholinesterase inhibitory properties, and molecular docking studies of heteroatom-containing sulfonyl hydrazone derivatives
AU - Celebioglu, Hasan Ufuk
AU - Erden, Yavuz
AU - Hamurcu, Fatma
AU - Taslimi, Parham
AU - Şentürk, Ozan Sanlı
AU - Özmen, Ümmühan Özdemir
AU - Tuzun, Burak
AU - Gulçin, İlhami
N1 - Publisher Copyright:
© 2020, © 2020 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2020
Y1 - 2020
N2 - 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.
AB - 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.
KW - Heteroatom
KW - antibacterial
KW - anticancer
KW - docking
KW - enzyme inhibition
KW - sulfonyl hydrazone
UR - http://www.scopus.com/inward/record.url?scp=85088393029&partnerID=8YFLogxK
U2 - 10.1080/07391102.2020.1792345
DO - 10.1080/07391102.2020.1792345
M3 - Article
C2 - 32691677
AN - SCOPUS:85088393029
SN - 0739-1102
SP - 1
EP - 12
JO - Journal of Biomolecular Structure and Dynamics
JF - Journal of Biomolecular Structure and Dynamics
ER -