Thienopyrazole derivatives have recently emerged as effective antitumoral agents with kinase inhibitory activity.  In this study, a novel thienopyrazole derivative with potent and selective in vitro cytotoxicity was identified in a high-throughput chemical library screening to identify novel anti-cancer drugs.  After 48 hours of exposure, compound Tpz-1 demonstrated potent and consistent cytotoxicity against a panel of human hematologic cells at nanomolar to low micromolar concentrations; an effect which was greatly diminished against the HS-27 non-cancerous foreskin fibroblast cell line.  Mechanistic analyses subsequently conducted against the CEM T-cell leukemia cell line revealed that Tpz-1 induces cell death via apoptosis and interferes with cell cycle progression in a dose-dependent manner.  These findings merit the further development of Tpz-1 as a novel therapeutic agent in the treatment of human hematologic cancers.

 

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