Environmentally Benign Copper Triflate-Mediated Multicomponent One-Pot Synthesis of Novel Benzo[g] chromenes Possess Potent Anticancer Activity

摘要

An efficient multi-component one-pot synthesis of highly functionalized 5,10-dihydro-4H-benzo[g]chromenes-3-caroni- trile derivatives from 2-hydroxy-1,4-naphthoquinone, aromatic aldehyde and malonitrile in the presence of Cu(OTf)_2 catalyst and eco friendly polyethylene glycol solvent was carried out under ultrasonication. The reaction was completed within 10 minutes and resulted in good yield. The synthesized com- pounds were tested for their in-vitro anticancer activity against cervical cancer cell line (HeLa). Nine out of ten compounds showed potent antitumor activity better than that of doxor- ubicin. 2-Amino-4-(3-methoxy-2-hydroxy)-5,10-dioxo-5,10-dihy- dro-4H-benzo[g]chromene-3-carbonitrile displayed highest ac- tivity among the test compounds and doxorubicin with IC_(50) equal to 1.27 μM.