Synthesis of [1,2]oxazolo[5,4-e]indazoles as antitumour agents

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.…”

(3,5-Dimethylpyrazol-1-yl)-[4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)phenyl]methanone

“…Compound 2 was the most active compound in this search with an IC50 equal to 7.5 nM [21]. In addition, the literature survey revealed that the pyrazole moiety represents an important pharmacophore in several anticancer active agents [22][23][24][25][26][27][28]. All these facts encouraged us to hybridize the pyrazolo [3,4-d] [29] with acetylacetone in acetic acid for 10 h, as shown in Scheme 1.…”

Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: In vitro antiproliferative activity and molecular mechanism(s) of action

“…Starting from our previous experience on polycondensed nitrogen heterocycles containing the pyrrole [8e14], indole [15e25] or indazole [26,27] moieties, with the aim to identify novel antitumor compounds, we extended our interest to the isoindole system [28e32]. Our efforts provided derivatives of the tetracyclic ring system isoindolo[2,1-a]quinoxaline (IIQ) which showed potent antiproliferative activity against the NCI human tumor cell lines panel with GI 50 values ranging from micromolar to nanomolar concentrations [33] and high activity on vinblastine and doxorubicin resistant cell lines.…”