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Site-Selective Rhodium(III)-Catalyzed C−H Amination of 7-Azaindoles with Anthranils: Synthesis and Anticancer Evaluation
- Source :
- Advanced Synthesis & Catalysis. 359:3471-3478
- Publication Year :
- 2017
- Publisher :
- Wiley, 2017.
-
Abstract
- The site-selective C–H amination reaction of 7-azaindoles with various benzisoxazoles as amination surrogates under cationic rhodium(III) catalysis is described. This transformation efficiently provides a range of ortho-aminated N-aryl-7-azaindoles with excellent site-selectivity and functional group compatibility. The formed ortho-aminated 7-azaindoles were readily transformed into biologically relevant heterocycles such as azaindoloacridine, azaindoloacridone, and bis-indole compounds. Moreover, the synthetic derivatives were tested for in vitro anticancer activity against human breast adenocarcinoma cells (MCF-7), human renal carcinoma cells (786-O), and human prostate adenocarcinoma cells (DU145). Notably, some synthetic compounds were found to display most potent anticancer activity, compared to that of anticancer doxorubicin as a positive control.
Details
- ISSN :
- 16154150
- Volume :
- 359
- Database :
- OpenAIRE
- Journal :
- Advanced Synthesis & Catalysis
- Accession number :
- edsair.doi...........5ac185db0bbe406afae0aed5a0426d19