European Journal of Medicinal Chemistry p. 648 - 660 (2015)
Update date:2022-08-15
Topics:
Spallarossa, Andrea
Caneva, Chiara
Caviglia, Matteo
Alfei, Silvana
Butini, Stefania
Campiani, Giuseppe
Gemma, Sandra
Brindisi, Margherita
Zisterer, Daniela M.
Bright, Sandra A.
Williams, Clive D.
Crespan, Emmanuele
Maga, Giovanni
Sanna, Giuseppina
Delogu, Ilenia
Collu, Gabriella
Loddo, Roberta
A new series of indole-based analogues were recently identified as potential anticancer agents. The Knoevenagel-type indoles herein presented were prepared via a one-pot condensation of iminium salts with active methylene reagents and were isolated as single geometric isomers. Biological evaluation in different cell-based assays revealed an antiproliferative activity for some analogues already in the nanomolar range against leukaemia, breast and renal cancer cell lines. To explain these effects, the most promising analogues of the series were engaged in further cell-based studies. Compounds 5e, l, p and 6a, b highlighted a pro-apoptotic potential being able to induce apoptosis in HL60, K562 and MCF-7 cell lines in a dose and time-dependent manner. The ability of these compounds to arrest cell cycle at the G2/M phase inspired the immunofluorescence studies which allowed us to identify tubulin as a potential target for compounds 5l and 6b.
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