Abstract A series of polysubstituted benzofuran derivatives was easily and rapidly prepared using a tandem Sonogashira coupling/cyclization reaction. Subsequent acylation afforded a small library of 39 new compounds that were assayed in cellulo on Plasmodium falciparum and Trypanosoma brucei parasites. Some of them exhibited good inhibitory activity on T. brucei proliferation.
[Farr, Roger N.; Alabaster, Ramon J.; Chung, John Y.L.; Craig, Bridgette; Edwards, John S.; Gibson, Andrew W.; Ho, Guo-Jie; Humphrey, Guy R.; Johnson, Simon A.; Grabowski Tetrahedron Asymmetry, 2003 , vol. 14, # 22 p. 3503 - 3515]
