Synthesis and antiproliferative activity of the ring system [1,2]oxazolo[4,5-g]indole

Abstract

Brand new ring: A series of 27 derivatives of the new ring system [1,2]oxazolo[4,5-g]indole were conveniently prepared and tested at the NCI for antiproliferative studies. Several of them showed good inhibitory activity toward all tested cell lines, reaching GI50 values generally at the micromolar and sub-micromolar levels and in some cases at nanomolar concentrations. The mean GI50 values, calculated on the full panel, were in the range 0.25-7.08 μM.

Keywords: [1,2]oxazolo[4,5-g]indoles; antiproliferative activity; combretastatin A-4; enaminoketones; hydroxylamine hydrochlorides.