Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D
Description
Protein kinase D (PKD) is a member of a novel family of serine/threonine kinases that regulate fundamental cellular processes. Investigators have developed a synthesis and biological evaluation of novel benzothienothiazepinone analogs. A ten-fold increase in the in vitro PKD1 inhibitory potency for the second generation lead kb-NB142-70 has been achieved. A transition to an almost equally potent novel pyrimidine scaffold has been accomplished. These promising results will guide the design of pharmacological tools to dissect PKD function and pave the way for the development of potential anti-cancer agents.
