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Chapter – 6 Biological evaluation of newly..... In case of DNJ-401 to DNJ-405, DNJ-405 was found to possess highest potency and lowest MIC value of 0.5 µg/ml against Bacillus pumilus MTCC 1607 while DNJ-404 was found to possess second lowest MIC value of 2 µg/ml and DNJ-403 was found to possess the MIC value of 4 µg/ml against the same bacterial strain. All these compounds were found to be moderate active against Staphylococcus epidermidis MTCC 155. DNJ-402 had good inhibitory effect on Staphylococcus pyogenes MTCC 442 with the MIC value of 4 µg/ml, where DNJ-401 and DNJ-404 were found to possess good antibacterial activity with MIC value of 4 µg/ml against Staphylococcus aureus MTCC 96. Rests of the compounds were found to be moderate active against all the bacterial strains. Thus the compounds possessing –CH2-CO group on nitrogen atom in indoline nucleus were found to be comparatively more active than the compounds possessing three carbon-alkyl chains on nitrogen atom in indoline nucleus. While the scenario was opposite in case of isatin moiety, where the compounds possessing three carbon-alkyl chains on nitrogen atom in isatin nucleus were found to be comparatively more active than the compounds possessing –CH2-CO group on nitrogen atom in isatin nucleus. In case of DNJ-501 to DNJ-505 only two compounds i.e. DNJ-501 and DNJ-505 were found to be good active against Bacillus pumilus MTCC 1607, Staphylococcus aureus MTCC 96 and Staphylococcus epidermidis MTCC 155 respectively with the MIC value of 4 µg/ml. Rests of the compounds were found to be moderate active against all the four bacterial strains. Results of antibacterial screening of DNJ-601 to DNJ-605 showed that only one compound DNJ-602 found to possess good antibacterial activity against Staphylococcus aureus MTCC 96 with the MIC value of 4 µg/ml. While rests of the compounds found to be moderate active against all the four bacterial strains. Department of Chemistry, Saurashtra University, Rajkot – 360 005 333
Chapter – 6 Biological evaluation of newly..... 6.2 CYTOTOXICITY ASSAY * Importance of 2-indolinone derivatives as anticancer and especially as tyrosine kinase inhibitors has been discussed in introduction part of Chapter – 3 under the title “Synthetic oxindoles as enzyme inhibitiors”. Thus indolinone derivatives (DNJ-1301 to DNJ-1305, DNJ-1401 to DNJ-1405 and DNJ-1501 to DNJ-1505) were screened in vitro for their cytotoxic activity at 1-100 µM concentration on a human stomach cancer cell line (Hu Tu 80), breast cancer cell line (MDA.MB.453) and lung cancer cell line (L132). Briefly, a three-day MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] in vitro cytotoxicity assay was performed. This test is based on the principle of uptake of MTT, a tetrazolium salt, by the metabolically active cells where it is metabolized by active mitochondria into a blue colored formazan product that is read spectrophotometrically. MTT was dissolved in phosphate buffered saline at a pH of 7.4 to obtain an MTT concentration of 5 mg/ml; the resulting mixture was filtered through a 0.22-mm filter to sterilize and remove a small amount of insoluble residue. A total of 10,000 cells were seeded in a 96-well culture plate and incubated with various concentrations of indolinone derivatives in a CO2 incubator for 72 hours. Control cells, not treated with indolinone derivatives were similarly incubated. The assay was terminated after 72 hours by adding 125 mg (25 ml) MTT to each well, followed by incubation for 3 hours, and finally added 50 ml of 10% SDS-0.01 N HCl to each well to lyse the cells and dissolve formazan. After incubating for 1 hour, the plate was read spectrophotometrically at 540 nm and the cytotoxicity percentage calculated using the formula: cytotoxicity percentage = (1-X/R1) x 100, where X = (absorbance of treated sample at 540 nm) - (absorbance of blank at 540 nm) and R1 = absorbance of control sample at 540 nm. Results of the cytotoxic assay for above mentioned compounds are summarized in the table given on the next page. * The results are obtained from Dabur Research Foundation, Ghaziabad. Department of Chemistry, Saurashtra University, Rajkot – 360 005 334
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Saurashtra University Re - Accredit
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Statement under O. Ph. D. 7 of Saur
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ACKNOWLEDGEMENT It is a moment of g
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Jignesh Lunagariya, Hitesh Sarvaiya
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CONTENT Content General Remarks 6 A
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Content 3.2 Reaction scheme 149 3.3
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5.14 Conclusion 313 5.15 Spectral r
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MF Molecular Formula MW Molecular W
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GABA Gamma Amino Butyric Acid MES M
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PART - A STUDIES ON 2-METHYL INDOLI
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Part-A Studies on 2-methyl indoline
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CHAPTER - 1 PREPARATION AND YIELD O
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Chapter - 1 Preparation and Yield o
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Part - B Studies on isatin derivati
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CHAPTER - 3 PREPARATION OF SMALL LI
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Chapter - 3 Preparation of small li
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CHAPTER - 4 STUDIES ON DIFFERENT TY
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Chapter - 4 Studies on different ty
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Chapter - 5 Synthesis and Character
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