Design, synthesis, and evaluation of potent bryostatin analogs that modulate PKC translocation selectivity.

ABSTRACT: Modern methods for the identification of therapeutic leads include chemical or virtual screening of compound libraries. Nature's library represents a vast and diverse source of leads, often exhibiting exquisite biological activities. However, the advancement of natural product leads into the clinic is often impeded by their scarcity, complexity, and nonoptimal properties or efficacy as well as the challenges associated with their synthesis or modification. Function-oriented synthesis represents a strategy to address these issues through the design of simpler and therefore synthetically more accessible analogs that incorporate the activity-determining features of the natural product leads. This study illustrates the application of this strategy to the design and synthesis of functional anal

SUBMITTER: Wender PA 

PROVIDER: S-EPMC3084132 | biostudies-literature | 2011 Apr

REPOSITORIES: biostudies-literature