Nafuredin (1) is converted to nafuredin-γ (2) under mild basic conditions and both compounds exhibit the same inhibitory activity and selectivity against NADH-fumarate reductase (complex I). The total synthesis of 2 was achieved by a convergent approach using Stille coupling. The structural elements required for inhibitory activity against NADH- fumarate reductase (complex I) were then investigated by evaluation of nafuredin-γ (2) ...