One-Pot Synthesis of Biheterocycles Based on Indole and Azole Scaffolds Using Tryptamines and 1,2-Diaza-1,3-dienes as Building Blocks

Abstract

The 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.

The incorporation of indole and azole pharmacophores into new biheterocyclic scaffolds as potential anticancer agents was achieved using different combinations of tryptamines, 1.2-diaza-1,3-dienes, aldehydes, and/or alkynes as readily available building blocks.

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