title: Antiproliferative and antibacterial activity of some glutarimide derivatives.
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.
authors.affiliation: a Department of Chemistry and Biochemistry and.
authors.forename: Jelena B
authors.initials: JB
authors.lastname: Popović-Djordjević
authors.affiliation: b Department for Industrial Microbiology, Faculty of Agriculture , University of Belgrade , Belgrade , Serbia .
authors.forename: Anita S
authors.initials: AS
authors.lastname: Klaus
authors.affiliation: c Institute of Oncology and Radiology of Serbia , Belgrade , Serbia , and.
authors.forename: Željko S
authors.initials: ŽS
authors.lastname: Žižak
authors.affiliation: c Institute of Oncology and Radiology of Serbia , Belgrade , Serbia , and.
authors.forename: Ivana Z
authors.initials: IZ
authors.lastname: Matić
authors.affiliation: d Department of Chemistry , Institute of Chemistry, Technology and Metallurgy, University of Belgrade , Belgrade , Serbia.
authors.forename: Branko J
authors.initials: BJ
authors.lastname: Drakulić
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D020014:K562 Cells; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D010881:Piperidones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D010881:Piperidones; C007864:glutarimide
keywords: Antitumor agents; heterocycles; structure–activity analysis