Synthesis and cytotoxic activity of some (+)-salsolidine derivatives.

On the basis of typical for secondary amino group reactions a number of derivatives of alkaloid (+)-salsolidine was synthesised. Cytotoxic properties of obtained compounds towards the HEK293, A549, MCF-7 and SH-SY5Y cell lines have been evaluated. As a result of the screening, the hit compound - 2-(chloroacetyl)-6,7-dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinoline () was identified, that inhibited the metabolic activity of A-549, MCF-7 and SH-SY5Y tumour cell lines with the IC values of 3.83 ± 0.78 µM, 5.84 ± 1.62 µM and 2.89 ± 0,92 µM correspondingly. Based on the effect of on the cell cycle progression and the molecular docking data, it was preliminary assumed that the cytotoxic activity of the can be realised through its interaction with the active site of the cyclin-dependent kinase CDK9 (PDB code 3BLR).