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 α-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 GI50 values from micro to submicromolar levels. Some of the new analogues exhibited good selectivities against different NCI sub-panels.

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

Anna Carbone
2022-01-01

Abstract

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 α-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 GI50 values from micro to submicromolar levels. Some of the new analogues exhibited good selectivities against different NCI sub-panels.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11567/1065440
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