864658-69-5Relevant articles and documents
Synthesis of non-THF analogs of acetogenin toward simplified mimics
Fujita, Daisuke,Ichimaru, Naoya,Abe, Masato,Murai, Masatoshi,Hamada, Takeshi,Nishioka, Takaaki,Miyoshi, Hideto
, p. 5775 - 5779 (2007/10/03)
Acetogenin analogs in which the bis-adjacent THF ring was replaced with an enantioselectively synthesized 1,2-cyclopentanediol bis-ether skeleton were synthesized to obtain simplified mimics, and their inhibitory effect on mitochondrial NADH-ubiquinone oxidoreductase (complex I) was examined. The results clearly demonstrate that the 1,2-cyclopentanediol bis-ether motif can substitute for the bis-THF ring while maintaining very potent inhibitory activity at the nanomolar level.