This paper has reviewed and compared the antioxidant and cytotoxicity properties of ethanol extracts of some Ayurvedic herbs, namely, Withania somnifera, Calotropis procera, and Semecarpus anacardium judged by the currently described pharmacological findings. The antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and a total phenolic content (TPC) test; cytotoxicity through the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay versus cultured tumor cell lines. Major differences in the bioactivity were observed: Calotropis procera and Semecarpus anacardium displayed high cytotoxic effects (IC 50 1.4-1.60g/mL), as reported in the literature. Withania somnifera exhibited moderate antioxidant potential, in vitro cytotoxicity (apoptotic and reactive oxygen species (ROS) generation seen in A549 lung carcinoma cellular models). The comparison analysis makes note of the therapeutic potential of the medicinal plants as sources of bioactive compounds that might be utilized in the drug development efforts by leveraging natural products and in their chemopreventive potential uses. Implications, limitations, and future research directions in studies are presented.