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.

New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

“…In the framework of our research on polycyclic nitrogen systems, [16,17,18,19,20,21,22,23,24,25,26,27,28,29,30,31,32,33] particularly referring to nortopsentin alkaloid analogues [34,35,36,37,38,39], herein we report the synthesis of the new series of thiazoles 1 (Table 1) and their evaluation as antibiofilm agents. In this series of nortopsentin analogues, the imidazole core of the natural product is replaced by the thiazole ring and one of the indole units is replaced by a 7-aza-indole moiety decorated with an ethanamine chain bound to the imine nitrogen.…”

Synthesis of substituted isoindolo[2,1-a]quinoxalin-6-yl–amino and 6-imino-5-yl thiourea derivatives

“…Quinoxalinylethylpyridylthioureas (QXPTs) of type 1 and 2 ( Figure 2) represent another class of NNRTIs; many compounds showed a potent activity against both HIV-1 wild-type RT and various HIV-1 mutants HIV-1 RT. 16 Considering the good experience reached in the course of our researches on polycyclic nitrogen systems, bearing pyrrole, [17][18][19][20][21][22][23][24] indole, [25][26][27][28][29][30][31][32][33][34][35] isoindole 36-38 and indazole …”

Synthesis and photocytotoxic activity of [1,2,3]triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines

“…Thus, as part of our search for nitrogen heterocycles [19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37] and considering that the antitumor effect of [1,6]naphthyridines has been widely investigated, but no examples of their photochemotherapeutic activity have been reported so far, herein we report the synthesis of the new ring systems [1,2,3]triazolo [4,5-h] [1,6]naphthyridines 5a-l, 7a-c, and [1,3]oxazolo [5,4h] [1,6]naphthyridines 6a-l, 8a-c with the aim of investigating their antiproliferative effect either in the dark and under light irradiation.…”