FR901464 is a cytotoxic natural product that binds splicing factor 3B subunit 1 (SF3B1) and PHD finger protein 5A (PHF5A), the components of the human spliceosome, to inhibit and alter the splicing of pre-mRNA. One thing that has halted its progression into the clinic is the poorly understood mechanism, or mode of inhibition, by this natural product. The left-hand tetrahydropyran ring of FR901464 binds SF3B1, and it remains unclear how the substituents on the ring contribute to the binding and three-dimensional conformation. We synthesized meayamycin D, an analog of FR901464, and three other analogs to probe the conformation through methyl scanning. This poster outlines the synthesis, conformational analysis, and biological evaluation of meayamycin D and its subsequent analogs.

Conformational analysis and biological evaluation of meayamycin

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