Anti-tumor Compounds Based on a Natural Product Consensus Pharmacophore

摘要

We report the design and highly enantioselective synthesis of a potent analog of the spliceosome inhibitor , based on a non-natural product scaffold. The design of this compound was facilitated by a pharmacophore hypothesis that assumed key interaction types that are common to and an otherwise unrelated natural product (pladienolide). The synthesis allows for the preparation of numerous novel analogs. We present results on the in vitro activity for this compound against several tumor cell lines.