Antiproliferative and antibacterial activity of some glutarimide derivatives
Članak u časopisu (Objavljena verzija)
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Taylor & Francis Group
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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.
Ključne reči:
Antitumor agents / heterocycles / structure–activity analysisIzvor:
Journal of Enzyme Inhibition and Medicinal Chemistry, 2016, 31, 915-923Izdavač:
- Taylor and Francis Ltd
Finansiranje / projekti:
- Proučavanje odnosa strukture i aktivnosti novosintetisanih biološki aktivnih supstanci (RS-172032)
- Modifikatori biološkog odgovora u fiziološkim i patološkim stanjima (RS-175011)
DOI: 10.3109/14756366.2015.1070844
ISSN: 1475-6366
PubMed: 26247353
WoS: 000385270300008
Scopus: 2-s2.0-84939214288
Institucija/grupa
IHTMTY - 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 . .