Cu(I)-Catalysis of One-Pot Synthesis of Some Novel Regioselective Isoxazole-Benzimidazole Hybrids and Their In Vitro Anti-Cancer Evaluation

Regioselective synthesis of some novel isoxazole-benzimidazole hybrids in high yields via Cu(I)-catalyzed tandem one-pot reaction of aromatic aldehydes with 1-prop-2-ynylbenzimidazole is developed. Structures of the synthesized compounds are confirmed by NMR and mass spectra. All the synthesized compounds have been tested for their in vitro anticancer activity against three human cancer cell lines including ACHN, MCF-7, and A375. Among these, three compounds demonstrate anticancer activity (0.54 to 4.21 mu M) higher than the positive control doxorubicin.