Figures & data
Scheme 1. The synthesis of the compounds (1–6).
Table 1. Cytotoxicity of compounds 1–6 against A549 cell line.
Table 2. Cytotoxicity of compounds 1–6 against C6 cell line.
Figure 1. DNA Synthesis inhibitory activity of compounds 1, 2, 4 and mitoxantrone on A549 cells. Mean percent absorbance of untreated control cells were assumed 0%. Three different concentrations (1a 31.2 µg/mL; 1b 62.5 µg/mL; 1c 125µg/mL; 2a 31.2 µg/mL; 2b 53.3 µg/mL; 2c 125 µg/mL; 4a 62.5 µg/mL; 4b 125 µg/mL; 4c 250 µg/mL; Mito a 7.8 µg/mL; Mito b 24.3 µg/mL; Mito c 31.2 µg/mL) of test compounds and mitoxantrone were given. Data points represent means for two independent experiments ± SD of four independent wells. p < 0.05.
Figure 2. DNA Synthesis inhibitory activity of compounds 1, 2, 4 and mitoxantrone on C6 cells. Mean percent absorbance of untreated control cells were assumed 0%. Three different concentrations (1a 31.2 µg/mL; 1b 50 µg/mL; 1c 125 µg/mL; 2a 31.2 µg/mL; 2b 45µg/mL; 2c 125 µg/mL; 4a 125 µg/mL; 4b 216 µg/mL; 4c 250 µg/mL; Mito a 3.9 µg/mL; Mito b 11 µg/mL; Mito c 15.6 µg/mL) of test compounds and mitoxantrone were given. Data points represent means for two independent experiments ± SD of four independent wells. p < 0.05.
Figure 3. Effect of Ac-DEVD-amc on the activity of caspase-3 induced by compounds 1, 2, 4 and mitoxantrone. A546 cells were maintained in cultures for 24 h and then exposed to Ac-DEVD-amc (1.0 mM) 30 min before exposure to 1a 31.2 µg/mL; 1b 86.7 µg/mL; 2a 31,2 µg/mL; 2b 53.3 µg/mL; 4a 62.5 µg/mL; 4b 193.3 µg/mL; Mito a 7.8 µg/mL; Mito b 24.3 µg/mL). Values represent mean ± S.D. from duplicate samples for each experiment. ***significantly different from respective control cells (p < 0.001).
Figure 4. Effect of Ac-DEVD-amc on the activity of caspase-3 induced by compounds 1, 2, 4 and mitoxantrone. C6 cells were maintained in cultures for 24 h and then exposed to Ac-DEVD-amc (1.0 mM) 30 min before exposure to (1a 31.2 µg/mL; 1b 50.7 µg/mL; 2a 31.2 µg/mL; 2b 45 µg/mL; 4a 125 µg/mL; 4b 216 µg/mL; Mito a 3.9 µg/mL; Mito b 11 µg/mL). Values represent mean ± S.D. from dublicate samples for each experiment.*: significantly different from respective control cells (p < 0.05).**significantly different from respective control cells (p < 0.01).***significantly different from respective control cells (p < 0.001).
Figure 5. Cellular and nuclear morphological changes of C6 cells following exposure to various concentrations of compound 1, 2, 4 and mitoxantrone for 24 h. (1b 50 µg/mL; 2b 45 µg/mL 4b 216 µg/mL; Mito b 11 µg/mL). Cells were distinguished according to the fluorescence emission and the morphological aspect of chromatin condensation in the stained nuclei. Viable cells have uniform bright green nuclei with organized structure. Early apoptotic cells have green nuclei, but perinuclear chromatin condensation is visible as bright green patches or fragments. White arrows indicate apoptotic cells.
