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A general synthesis of arylindoles and (1-arylvinyl)carbazoles via a one-pot reaction from N-tosylhydrazones and 2-nitro-haloarenes and their potential application to colon cancer.

Tourin BzeihTimothée NaretAli HachemNada JaberAli KhalafJerome BignonJean-Daniel BrionMouad AlamiAbdallah Hamze
Published in: Chemical communications (Cambridge, England) (2018)
A convergent and effective synthesis of 3-aryl-indoles, 2,3-diaryl indoles, and (1-arylvinyl)carbazoles from a one-pot sequence involving the coupling of N-tosylhydrazones with ortho-nitro-haloarenes followed by a cyclization has been developed. Compound 5i exhibits excellent antiproliferative activity in the low nM range against colon cancer cell lines.
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