E. Sailaja, S. Bhavani, D. Rambabu
Dec 14, 2015
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Journal
Arabian Journal of Chemistry
Abstract
Abstract In view of known antitumor and cytotoxic properties of 2- and 3-pyridinyl substituted indole derivatives, respectively a number of isomeric N -pyridinyl substituted indoles and their analogs were synthesized as potential cytotoxic agents. A greener approach was developed to synthesize these compounds via an ultrasound assisted selective N − 1 heteroarylation of indoles. The methodology involved reaction of indoles with heteroaryl halides in PEG-400 under ultrasound irradiation. One of the products i.e. 1-(pyrimidin-2-yl)-1 H -indole was further functionalized via Pd-mediated C H activation at C-2 on the indole ring. All the synthesized N − 1 heteroarylindoles were tested for their in vitro anti-proliferative properties against cancer (leukemia) and non-cancerous cell lines. Some of the compounds showed promising and selective cytotoxic effects toward leukemia cells.