LAUSR

Combination of cyclin‐dependent kinases (CDKs) and histone deacetylases (HDACs) inhibitors may have statistical synergy in suppressing cancer cell proliferation. Herein, a novel CDKs/HDACs dual inhibitor T‐17 was rationally designed, synthesized, and evaluated. Our results demonstrated that T‐17 concurrently exhibited potent and balanced inhibitory activity against CDKs (IC50 = 18.0 nM) and HDACs (IC50 = 6.6 nM) and also displayed good cell viability inhibitory effect on four cancer cell lines. Meanwhile, T‐17 blocked the MDA‐MB‐231 and A549 cell cycle at G1 phase and S phase, respectively. In addition, T‐17 induced MDA‐MB‐231 cells apoptosis and inhibited the HDACs and CDKs mediated signaling pathways. Finally, we also found that T‐17 had good antitumor activity in vivo. In summary, these results indicated that T‐17 would be a promising lead compound which deserves further research.