Synthesis of 1-indolyl substituted β-carboline natural products and discovery of antimalarial and cytotoxic activities

• DOI: 10.1016/j.tet.2014.05.068
• Publication Date: 2014-05-24T07:31:50Z
• Authors: Lydia P.P. Liew; Jessica M. Fleming; Arlette Longeon; Elisabeth Mouray; Isabelle Florent; Marie-Lise Bourgu...; Brent R. Copp
• Keywords: Tryptamines; IC50; Antimalarial Agent; Aldol condensation; Cancer cell lines; Structure–activity relationship

AbstractA series of 1‐indolyl substituted β‐carbolines including the natural products hyrtiosulawesine (Ia), pityriacitrin (Ib) and pityriacitrin B (Ic) are prepared via a Pictet—Spengler condensation‐oxidation strategy from the corresponding indolyl aldehydes and substituted tryptamines.