CER - Central Repository
Institute of Chemistry, Technology and Metallurgy
    • English
    • Српски
    • Српски (Serbia)
  • English 
    • English
    • Serbian (Cyrillic)
    • Serbian (Latin)
  • Login
View Item 
  •   CER
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
  •   CER
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

Antiproliferative and antibacterial activity of some glutarimide derivatives

Thumbnail
2016
bitstream_6327.pdf (831.0Kb)
Authors
Popović-Đorđević, Jelena B.
Klaus, Anita
Žižak, Željko
Matić, Ivana Z.
Drakulić, Branko
Article (Published version)
,
Taylor & Francis Group
Metadata
Show full item record
Abstract
Antiproliferative and antibacterial activities of nine glutarimide derivatives (1–9) were reported. Cytotoxicity of compounds was tested toward three human cancer cell lines, HeLa, K562 and MDA-MB-453 by MTT assay. Compound 7 (2-benzyl-2-azaspiro[5.11]heptadecane-1,3,7-trione), containing 12-membered ketone ring, was found to be the most potent toward all tested cell lines (IC50 = 9–27 μM). Preliminary screening of antibacterial activity by a disk diffusion method showed that Gram-positive bacteria were more susceptible to the tested compounds than Gram-negative bacteria. Minimum inhibitory concentration (MIC) determined by a broth microdilution method confirmed that compounds 1, 2, 4, 6–8 and 9 inhibited the growth of all tested Gram-positive and some of the Gram-negative bacteria. The best antibacterial potential was achieved with compound 9 (ethyl 4-(1-benzyl-2,6-dioxopiperidin-3-yl)butanoate) against Bacillus cereus (MIC 0.625 mg/mL; 1.97 × 10−3 mol/L). Distinction between more and... less active/inactive compounds was assessed from the pharmacophoric patterns obtained by molecular interaction fields.

Keywords:
Antitumor agents / heterocycles / structure–activity analysis
Source:
Journal of Enzyme Inhibition and Medicinal Chemistry, 2016, 31, 915-923
Publisher:
  • Taylor and Francis Ltd
Funding / projects:
  • Structure-activity relationship of newly synthesized biological active compound (RS-172032)
  • Biological response modifiers in physiological and pathological conditions (RS-175011)

DOI: 10.3109/14756366.2015.1070844

ISSN: 1475-6366

PubMed: 26247353

WoS: 000385270300008

Scopus: 2-s2.0-84939214288
[ Google Scholar ]
9
5
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/2667
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - JOUR
AU  - Popović-Đorđević, Jelena B.
AU  - Klaus, Anita
AU  - Žižak, Željko
AU  - Matić, Ivana Z.
AU  - Drakulić, Branko
PY  - 2016
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/2667
AB  - Antiproliferative and antibacterial activities of nine glutarimide derivatives (1–9) were reported. Cytotoxicity of compounds was tested toward three human cancer cell lines, HeLa, K562 and MDA-MB-453 by MTT assay. Compound 7 (2-benzyl-2-azaspiro[5.11]heptadecane-1,3,7-trione), containing 12-membered ketone ring, was found to be the most potent toward all tested cell lines (IC50 = 9–27 μM). Preliminary screening of antibacterial activity by a disk diffusion method showed that Gram-positive bacteria were more susceptible to the tested compounds than Gram-negative bacteria. Minimum inhibitory concentration (MIC) determined by a broth microdilution method confirmed that compounds 1, 2, 4, 6–8 and 9 inhibited the growth of all tested Gram-positive and some of the Gram-negative bacteria. The best antibacterial potential was achieved with compound 9 (ethyl 4-(1-benzyl-2,6-dioxopiperidin-3-yl)butanoate) against Bacillus cereus (MIC 0.625 mg/mL; 1.97 × 10−3 mol/L). Distinction between more and less active/inactive compounds was assessed from the pharmacophoric patterns obtained by molecular interaction fields.
PB  - Taylor and Francis Ltd
T2  - Journal of Enzyme Inhibition and Medicinal Chemistry
T1  - Antiproliferative and antibacterial activity of some glutarimide derivatives
VL  - 31
SP  - 915
EP  - 923
DO  - 10.3109/14756366.2015.1070844
ER  - 
@article{
author = "Popović-Đorđević, Jelena B. and Klaus, Anita and Žižak, Željko and Matić, Ivana Z. and Drakulić, Branko",
year = "2016",
abstract = "Antiproliferative and antibacterial activities of nine glutarimide derivatives (1–9) were reported. Cytotoxicity of compounds was tested toward three human cancer cell lines, HeLa, K562 and MDA-MB-453 by MTT assay. Compound 7 (2-benzyl-2-azaspiro[5.11]heptadecane-1,3,7-trione), containing 12-membered ketone ring, was found to be the most potent toward all tested cell lines (IC50 = 9–27 μM). Preliminary screening of antibacterial activity by a disk diffusion method showed that Gram-positive bacteria were more susceptible to the tested compounds than Gram-negative bacteria. Minimum inhibitory concentration (MIC) determined by a broth microdilution method confirmed that compounds 1, 2, 4, 6–8 and 9 inhibited the growth of all tested Gram-positive and some of the Gram-negative bacteria. The best antibacterial potential was achieved with compound 9 (ethyl 4-(1-benzyl-2,6-dioxopiperidin-3-yl)butanoate) against Bacillus cereus (MIC 0.625 mg/mL; 1.97 × 10−3 mol/L). Distinction between more and less active/inactive compounds was assessed from the pharmacophoric patterns obtained by molecular interaction fields.",
publisher = "Taylor and Francis Ltd",
journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",
title = "Antiproliferative and antibacterial activity of some glutarimide derivatives",
volume = "31",
pages = "915-923",
doi = "10.3109/14756366.2015.1070844"
}
Popović-Đorđević, J. B., Klaus, A., Žižak, Ž., Matić, I. Z.,& Drakulić, B.. (2016). Antiproliferative and antibacterial activity of some glutarimide derivatives. in Journal of Enzyme Inhibition and Medicinal Chemistry
Taylor and Francis Ltd., 31, 915-923.
https://doi.org/10.3109/14756366.2015.1070844
Popović-Đorđević JB, Klaus A, Žižak Ž, Matić IZ, Drakulić B. Antiproliferative and antibacterial activity of some glutarimide derivatives. in Journal of Enzyme Inhibition and Medicinal Chemistry. 2016;31:915-923.
doi:10.3109/14756366.2015.1070844 .
Popović-Đorđević, Jelena B., Klaus, Anita, Žižak, Željko, Matić, Ivana Z., Drakulić, Branko, "Antiproliferative and antibacterial activity of some glutarimide derivatives" in Journal of Enzyme Inhibition and Medicinal Chemistry, 31 (2016):915-923,
https://doi.org/10.3109/14756366.2015.1070844 . .

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

re3dataOpenAIRERCUB
 

 

All of DSpaceInstitutions/communitiesAuthorsTitlesSubjectsThis institutionAuthorsTitlesSubjects

Statistics

View Usage Statistics

DSpace software copyright © 2002-2015  DuraSpace
About CeR – Central Repository | Send Feedback

re3dataOpenAIRERCUB