Design, Synthesis and Biological Evaluation of Thiazolidine-2,4-dione-biphenyl Derivatives as Anticancer Agents.

OBJECTIVE: A new library of Thiazolidine-2,4-dione-biphenyl Derivatives derivatives (10a-j) was designed and synthesized. All compounds were characterized by spectral data. Further, these were evaluated for their in vitro anticancer activity. METHODS: The compounds were synthesized as planned in the Scheme-1 and compounds were screened against four human cancer cell lines like cervical cancer (Hela), prostate cancer (PC3), lung cancer cells and breast cancer cells (MDA-MB-231) by employing of MTT assay. Doxorubicin was chosen as positive control. RESULT: Most of the compounds showed moderate to good activity. Among them, these compounds 10b and 10d and displayed more potent activity. Predominantly, one compound 10d showed remarkable anticancer activity. Molecular docking studies with EGFR target (PDB ID: 1M17) exhibits compounds 10b and 10d showed desirable molecular interactions with the same residue similar to cocrystal ligand Erlotinib. CONCLUSION: This results indicate that these two compounds are well targeted the EGFR active sites and showed more inhibitory effects than the other compounds.