Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents-Synthesis, In Vitro and In Silico Studies.

A series of 2-(1-indol-2-yl)-3-acrylonitrile derivatives, -, , -, -, -, and , were synthesized as potential antitumor and antimicrobial agents. The structures of the prepared compounds were evaluated based on elemental analysis, IR, H- and NMR, as well as MS spectra. X-ray crystal analysis of the representative 2-(1-indol-2-yl)-3-acrylonitrile showed that the acrylonitrile double bond was -configured.

1-[(Imidazolidin-2-yl)imino]-1H-indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies.

A series of 1-[(imidazolidin-2-yl)imino]-1H-indole analogues of hypotensive α -AR agonists, 1-[(imidazolidin-2-yl)imino]-1H-indazoles, was synthesized and tested in vitro for their activities at α - and α -adrenoceptors as well as imidazoline I and I receptors. The most active 1-[(imidazolidin-2-yl)imino]-1H-indoles displayed high or moderate affinities for α - and α -adrenoceptors and substantial selectivity for α -adrenoceptors over imidazoline-I binding sites. The in vivo cardiovascular properties of indole derivatives 3 revealed that substitution at C-7 position of the indole ring may result in compounds with high cardiovascular activity.