Tranilast-tyrosine hybrid molecule exhibits dual activity: suppression of epithelial-mesenchymal transition and induction of cytotoxicity in cancer cells

The anti-allergic drug tranilast (TNL) reportedly exhibits inhibitory activity against epithelial-mesenchymal transition (EMT) at high concentrations. Herein, we synthesized a new hybrid molecule, tyrosine-conjugated TNL having propyl linker (TNL-T), which is expected to increase anti-EMT by enhancing intracellular delivery through an amino acid transporter expressed in cancer cells. of TNL-T was similar that the lung carcinoma cell line A549. Unlike TNL, could induce dose-dependent cytotoxicity A549 cells; this also observed glioblastoma lines U251 and U87. However, neither tyrosine nor exhibited such cytotoxicity, demonstrating importance structure. derivatization study showed derivative with ethyl has functions, pentyl inactive. TNL-T, dual suppressing EMT proliferation, aid development anticancer drugs.