Donwload Design, Synthesis and Docking study of N-substituted 2,4- Thiazolidinedione as Cytotoxic Agents

SUMMARY

Download Design, Synthesis and Docking study of N-substituted 2,4- Thiazolidinedione as Cytotoxic Agents

·         Introduction about anticancer agents have been studied.

·         Chemistry and biological importance of 2,4-thiazolidinedione have also been studied.

·         Various literatures regarding N-substituted 2,4-thiazolidinedione with biological activity have been reviewed.

·         Docking study on the ERK2 receptor has been done by AUTODOCK 4.2 software. And 132 compounds were predicted.

·         Different 8 good docking scoring  N-substituted 5-arylidine 2,4-thiazolidinedione derivatives have been synthesized.

·         All the synthesized compounds were characterized by IR, Mass and 1H NMR spectroscopy.

·         MTT solution (5 mg/ml in phosphate buffered saline (PBS) pH 7.5), HCl, Propan-2-ol  96-well micro titer plate, ELISA reader.

·         The in vitro cytotoxic activity were performed against human carcinoma cell lines: NCI-H292 (obtained from muco epidermoid carcinoma of lung), HEp-2 (obtained from epidermoid carcinoma of the larynx), MDA MB-231(brest cancer cell line), A375( human melanoma cell line).

·         Normal cell line : HEK 293P

·         X 104  Cell were grown in micro titer plates in a final volume of 100 µl culture medium per well. Cells were incubated for 24 hr at 37˚C & 5% CO2.

·         Various amounts of compound were added (final concentration e.g. 100µM - 0.005µM) into micro plates (96 wells, flat bottom).

·         After incubation period, 10 µL of the MTT labeling mixture were added.

·         Plate was allowed for incubation 4 hr at 37˚C under CO2 incubator.

·         Then 100 µl solubilization solution were added.

·         Absorbance were measured with use Microplate reader at 590 nm (reference wavelength of 650 nm).

·         Thesis is under process by Dhaval Shah.