In vitro and in vivo activity of novel platinum(<scp>ii</scp>) complexes with naphthalene imide derivatives inhibiting human non-small cell lung cancer cells

Four new Pt(II) complexes, [Pt(La)]Cl (1), [Pt(Lb)]Cl (2), [Pt(Lc)]Cl (3) and [Pt(Ld)]Cl (4) with the naphthalene imide derivatives La–Ld as ligands were designed and prepared. MTT assay indicated that 1–4 exhibited proliferation inhibiting activity against human non-small cell lung cancer (NCI-H460) cells, especially 1–3 showed superior activity (IC50 = 0.10–8.56 μM) compared with cisplatin (IC50 = 12.01 &#177; 1.03 μM). Various experiments showed that 3 as a telomerase inhibitor induced NCI-H460 cell apoptosis via inhibition of the telomerase and dysfunction of mitochondria. In vivo evaluation results suggested that 3 could significantly inhibit the growth of tumor cells in NCI-H460 tumor-bearing mice and the tumor growth inhibition rate (TGI) reached 40.7%. These results demonstrated that 3 is a telomerase inhibitor and a promising anti-cancer agent.