Synthesis and Invitro Anti-Cancer Evaluation of Some Novel 2, 3 Disubstituted Thiazolidinones

AIM AND OBJECT: the present study are, To synthesize a series of novel 2, 3-disubstituted thiazolidinones. To characterize the synthesized compounds by IR, NMR, Mass spectra and elemental analysis. To evaluate the test compounds for anti-cancer activity by using human cervical cancer cell line (HeLa) by MTT assay method.SUMMARY AND CONCLUSION:In summary, a new series of 2-(3-(4-(4-aminophenylsulfonyl) phenyl)-4-oxo-2-(4- substituted-phenyl thiazolidin-5-yl) acetic acid were synthesized. These title compounds containing seven different substituents at C-2 and C-3 were screened for their anticancer agents. Most of the test compounds were found to exhibit significant anticancer activity against the human cervical cancer cell line (HeLa) in the highest concentration. Among the substituents at C-2, p-chloro phenyl substituent and at C-5 4-amino phenyl sulfonyl substitutent showed maximum potency, while 4-methoxy phenyl, 4- hydroxy phenyl and 4- nitro phenyl substitutent showed equipotent activity but the dimethylaminophenyl, vinyl and 4-amino phenyl substituent at C-2 exhibited least activity when compare to other substituents. The order of activity at C-2 is p-chloro phenyl ≥ 4- hydroxy phenyl ≥ 4-methoxy phenyl ≥ 4- nitro phenyl ≥ 4-amino phenyl ≥ dimethylaminophenyl ≥ vinyl substituents. Among the test compounds, compound 3-(4-(4-aminophenylsulfonyl)phenyl)-2-(4- chlorophenyl)-4-oxothiazolidin-5-yl) acetic acid (TD7) was found to be the most active agent which showed 74.85 percentage of cell inhibition against the human cervical cancer cell line (HeLa) in the highest concentration, which have p-chlorophenyl group in the thiazolidinone nucleus. Hence this molecule can be selected as a lead molecule of the present study for further exploitation