LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC50s of 2.99 and 2.47 µM, respectively.
LQZ-7F could be hudrolyzed under acidic conditions[1].LQZ-7F (2.5 μM, 72 hours) displays cytotoxicity towards human cancer cells (PC-3, C4-2) with the IC50s of 2.99 μM and 2.74 μM, respectively[1].LQZ-7F effectively inhibits survival of all cancer cell lines with IC50 values ranging between 0.4 and 4.4 mM[2].LQZ-7F (2 μM, 24 hours) disrupts microtubule structure and cause mitotic arrest in P3 cells[2].
LQZ-7F (i.p. injection; 25 mg/kg once every 3 days; 24 days) inhibits growth of xenograft tumor and may be due to its induction of surviving degradation in vivo[1].
References:
[1]. Robert Peery, et al. A novel survivin dimerization inhibitor without a labile drazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells. Bioorg Med Chem.2022 Jul 1;65:116761.
[2]. Qi Jing, et al. Effective Targeting of the Survivin Dimerization Interface with Small-Molecule Inhibitors. Cancer Research. 2016 Jan. 76(2):453-462.