91123-59-0Relevant academic research and scientific papers
Unconventional Knoevenagel-type indoles: Synthesis and cell-based studies for the identification of pro-apoptotic agents
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
, p. 648 - 660 (2015/09/07)
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.
Scandium-catalyzed intramolecular friedel-crafts reactions of 2-[(2-Alkyl-1 H -indol-3-yl)methylene]malonates
Oh, Chang Ho,Park, Hyo Seung,Park, Nari,Kim, So Young,Piao, Lanhua
, p. 579 - 585 (2014/03/21)
We have synthesized a variety of 2-[(2-alkyl-1H-indol-3-yl)methylene] malonates and studied their scandium-catalyzed intramolecular Friedel-Crafts reactions leading to the corresponding polycyclic compounds such as indeno[1,2-b]indoles and benzo[1,2-b]carbazoles. Georg Thieme Verlag Stuttgart New York.
