partially_open7noThe rapid and expedient assembly of three new classes of biheterocycles of biological interest, viz. indole–imidazoles 4, indole–pyrroles 6 and indole–triazoles 8 was accomplished using different combinations of tryptamines, 1,2-diaza-1,3-dienes, aldehydes, and/or alkynes as readily available building blocks. Twenty-six derivatives were thus prepared in excellent yields (up to 100 %). The products were screened for in-vitro biological studies. Some of these revealed promising anticancer activity against MCF7 and Caco-2 human tumor cell lines.mixedMantenuto, Serena; Lucarini, Simone; De Santi, Mauro; Piersanti, Giovanni; Brandi, Giorgio; Favi, Gianfranco; Mantellini, FabioMantenuto, Serena; Lucarini, Simone; DE SANTI, Mauro; Piersanti, Giovanni; Brandi, Giorgio; Favi, Gianfranco; Mantellini, Fabi