CER - Central Repository
Institute of Chemistry, Technology and Metallurgy
    • English
    • Српски
    • Српски (Serbia)
  • English 
    • English
    • Serbian (Cyrilic)
    • Serbian (Latin)
  • Login
View Item 
  •   Central Repository
  • IHTM
  • Radovi istraživača / Researchers' publications
  • View Item
  •   Central Repository
  • 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
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 ]
4
3
URI
http://cer.ihtm.bg.ac.rs/handle/123456789/2667
Collections
  • Radovi istraživača / Researchers' publications
Institution
IHTM

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

OpenAIRERCUB
 

 

All of DSpaceInstitutionsAuthorsTitlesSubjectsThis institutionAuthorsTitlesSubjects

Statistics

View Usage Statistics

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

OpenAIRERCUB