Synthesis of Simplified Discodermolide Analogs

摘要

Discodermolide was discovered in 1990 and with its discovery set off an expansiveudmedicinal chemistry program fueled by many groups’ research. It acts as a microtubuleudstabilizer, which makes it a potential anti-cancer agent. The synthesis of simplifieduddiscodermolide analogs is reported here. These analogs use simplified versions of the lactoneudand carbamate fragments, which are then coupled via olefin metathesis. Hologram quantitativeudstructure-activity relationship (HQSAR) is also used to show that an olefin linker inserted byudolefin metathesis as viable simple alternatives to the complex middle portion usually found in theudparent molecule.