Bioactive 4-substituted-6-methyl-2-pyrones with promising cytotoxicity against A2780 and K562 cell lines

Bioorganic and Medicinal Chemistry Letters

Volumn 12, Issue 24, 2002, Pages 3509-3513

  Marrison, Lester R ^a   Dickinson, Julia M ^a   Fairlamb, Ian J S ^a,b  

^a MANCHESTER METROPOLITAN UNIVERSITY   (United Kingdom)

^b UNIVERSITY OF YORK   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; CARBON; PALLADIUM; PYRONE DERIVATIVE; ANTIINFECTIVE AGENT;

ANTIMICROBIAL ACTIVITY; ARTICLE; CANCER CELL CULTURE; CATALYSIS; CATALYST; CELL STRAIN K 562; CHEMICAL BOND; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG POTENCY; DRUG SCREENING; HUMAN; HUMAN CELL; NONHUMAN; STEREOCHEMISTRY; BACTERIUM; CELL CULTURE; CELL DIVISION; DRUG EFFECT; FUNGUS; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ANTI-BACTERIAL AGENTS; ANTI-INFECTIVE AGENTS; ANTINEOPLASTIC AGENTS; BACTERIA; CELL DIVISION; FUNGI; HUMANS; PYRONES; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED;

EID: 0036890401     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(02)00824-7     Document Type: Article

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27. 2 atmosphere for 5 days. After incubation, 50 μL of MTT solution (3 mg/mL) was added to each well and the plate returned to the incubator for 3 h. After this time, the medium and excess MTT was aspirated from each well and the formazan crystals were solubilised in 200 μL of DMSO. The plate was then read using a multiscan microplate reader (Titretech, Labsystems UK Ltd) at 540 nm with subtraction at 620 nm to allow for turbidity. The resultant output was processed and the percentage growth inhibition for each dose calculated, each experiment was performed in duplicate. Mean and standard deviations for each dose were calculated from duplicate experiments. Based on a standard assay: Mossmann T. J. Immunol. Methods. 63:1983;55 (b) Edmondson J.M., Armstrong L.S., Martinez A.O. J. Tissue Culture Methods. 11:1988;15.
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29. A variety of E-chalcones have been reported with potent inhibitory activity against the K562 cell line, see: Ducki S., Forrest R., Hadfield J.A., Kendall A., Lawrence N.J., McGown A.T., Rennison D. Bioorg. Med. Chem. Lett. 8:1998;1051. For references relating to inhibitory activity against the A2780 cell line, see: (a) McClusky A., Bowyer M.C., Collins E., Sim A.T.R., Sakoff J.A., Baldwin M.L. Bioorg. Med. Chem. Lett. 10:2000;1687 (b) Kokotos G., Constantinou-Kokotou V., Padrón J.M., Peters G.J. Bioorg. Med. Chem. Lett. 11:2001;861.
30. A variety of E-chalcones have been reported with potent inhibitory activity against the K562 cell line, see: Ducki S., Forrest R., Hadfield J.A., Kendall A., Lawrence N.J., McGown A.T., Rennison D. Bioorg. Med. Chem. Lett. 8:1998;1051. For references relating to inhibitory activity against the A2780 cell line, see: (a) McClusky A., Bowyer M.C., Collins E., Sim A.T.R., Sakoff J.A., Baldwin M.L. Bioorg. Med. Chem. Lett. 10:2000;1687 (b) Kokotos G., Constantinou-Kokotou V., Padrón J.M., Peters G.J. Bioorg. Med. Chem. Lett. 11:2001;861.
31. (a) An antibiotic 'ring', which contained several known potent anti-bacterial agents (Novobiocin, Penicillin G, Streptomycin, Tetracyline, Chloroamphenicol, Erythromycin, Fusidic acid and Methicillin), was used as the control in the bacterial assays (individual discs contain 1 unit). Zones of inhibition (∼5-8 mm) were observed for these compounds. (b) Squalestatin S1 (Zaragozic acid A), an extremely potent yeast inhibitor, was used as a control in the yeast assay (200 μg/disk). The zones of inhibition observed against C. albicans, S. cerevisiae and S. pombe were 27, 27 and 37 mm, respectively.
32. 2O to give a final concentration of 200 μg/disk.