Azo-directed rhodium(III)-catalysed C–H functionalization and intramolecular annulation reactions between azobenzenes and internal olefins are described. This transformation leads to 2,3-disubstituted free (NH)-indoles with excellent site-selectivity and functional-group compatibility. The resulting indoles were evaluated for in-vitro anticancer activity against human endometrial adenocarcinoma cells (Ishikawa), triple negative human breast cancer cells (MDA-MB-231), and human renal cancer cells (Caki-1). 2,3-Disubstituted indoles 3b, 3k, and 5b were found to show potent cytotoxic effects that were competitive with the anticancer agent doxorubicin.Wednesday, October 25, 2017
Synthesis and Anticancer Evaluation of 2,3-Disubstituted Indoles Derived from Azobenzenes and Internal Olefins: EJOC 2017
Azo-directed rhodium(III)-catalysed C–H functionalization and intramolecular annulation reactions between azobenzenes and internal olefins are described. This transformation leads to 2,3-disubstituted free (NH)-indoles with excellent site-selectivity and functional-group compatibility. The resulting indoles were evaluated for in-vitro anticancer activity against human endometrial adenocarcinoma cells (Ishikawa), triple negative human breast cancer cells (MDA-MB-231), and human renal cancer cells (Caki-1). 2,3-Disubstituted indoles 3b, 3k, and 5b were found to show potent cytotoxic effects that were competitive with the anticancer agent doxorubicin.
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