Tetrahedron p. 1785 - 1801 (2018)
Update date:2022-08-03
Topics: Acridines
Brikci-Nigassa, Nahida Mokhtari
Bentabed-Ababsa, Ghenia
Erb, William
Chevallier, Floris
Picot, Laurent
Vitek, Lucille
Fleury, Audrey
Thiéry, Valérie
Souab, Mohamed
Robert, Thomas
Ruchaud, Sandrine
Bach, Stéphane
Roisnel, Thierry
Mongin, Florence
Because N-arylation of isatin only worked with iodoferrocene (and in low yield), we employed N-arylation of 2-aminophenones and subsequent oxidative cyclization to access various N-arylated isatins. In the course of this work, we observed that N-arylation using 2-iodofuran, 2-iodobenzofuran and 2-iodobenzothiophene did not lead to the expected derivatives, but to (benzo)furo- and (benzo)thieno[2,3-b]quinolines. Separate cyclization was also performed under acidic conditions on 2-(arylamino)phenones in order to obtain acridines and related compounds. Most of the synthesized compounds were screened for their antiproliferative activity in A2058 melanoma cells, and against a panel of disease-relevant kinases such as mammalian CDK5/p25, PIM1, CLK1, DYRK1A, GSK3α/β Haspin and leishmanial CK1. The biological results are reported.
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