Hybrid probes of aromatic amine and barbituric acid: highly promising leads for anti-bacterial, anti-fungal and anti-cancer activities

Abstract

Today, cancer and resistant microbes remain one of the most deadly diseases in the world. In search of novel anti-cancer and anti-microbial probes, a series of newly hybrid molecules is synthesized by combining the structural features of aromatic amines and barbituric acid, using the concept of green chemistry. This approach was accomplished efficiently using water as the greener solvent and in the absence of catalyst to give the corresponding adducts. All newly synthesized compounds were characterized by spectral analysis FT-IR, ¹H NMR, ¹³C NMR, HMBC and Elemental Analysis. Evaluations of these probes over four human cancer cell lines (Breast adenocarcinoma cancer cell line MCF-7, Non-small cell lung cancer cell line NCI-H460, CNS cancer cell line SF-268 and fibroblast cancer cell line WI-38), anti-microbial activity against five bacterial strains (S. pyogenes MTCC 442 and S. aureus MTCC 96 as the gram positive, E. coli MTCC 443, P. aeruginosa MTCC 424 and K. pneumoniae MTCC 109 as the gram negative) and four fungal strains (C. albicans MTCC 227, A. clavatus MTCC 1323, T. rubrum MTCC 296 and Penicillium wild strain). Out of set of nineteen probes, three probes show significant anti-cancer activities against MCF-7, NCI-H460 and SF-268, whereas sixteen probes exhibit potent anti-tumour activity against WI-38 cell lines. Within anti-microbial bioassay, three molecules exhibited significant activity against both the gram-positive as well as gram-negative bacteria, whereas two compounds showed highly potent activity against T. rubrum fungi, while three molecules were found to be equipotent against T. rubrum as a fungal strain.