Synthesis and cytotoxic activity of 3-[2-(1H-Indol-3-yl)-1,3-thiazol-4-yl]-1H-pyrrolo[3,2-c]pyridine hydrobromides, analogues of the marine alkaloid nortopsentin

A new series of thiazole nortopsentin analogues with a 5-azaindole moiety was conveniently synthesized in good to excellent yields by an Hantzsch reaction between thioamides and alpha-bromoacetyl compounds. The cytotoxic activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. All tested compounds were active against all of the investigated cell lines showing GI(50) values from micro to submicromolar levels. Some of the new analogues exhibited good selectivities against different NCI sub-panels. [GRAPHICS] .

Automated summary

A series of thiazole nortopsentin analogues with a 5-azaindole moiety were synthesized conveniently and showed cytotoxic activity against different human tumor cell lines.