The elucidation of structures and functions of plant derived natural products having various biological properties plays a vital role in treating several lethal diseases. This review mainly focuses on the study of rarely explored plants and their compounds which have been scientifically proved to be prospective anticancer agents. Existing cytotoxic drugs affects rapidly dividing cells without adequate differentiation of normal and cancerous cells, it also damages the normal tissues. So the strategies for discovering cancer drug mainly reflect on targeting specific proteins implicated in tumour growth and progression. As the use of phytochemicals are promising and escalating rapidly, the appropriate scientific study to extract bioactive chemicals, detail assessment of its role in anticancer treatment and clinical studies might be the appealing issue of upcoming cancer research. This review summarizes proof of benefits by presenting the list of non-toxic and prevailing natural sources of drugs for patients who are in need. Thus, it is worthwhile to overview the traditional and current status on the usage of bioactive compounds in anticancer activity. © 2016, Research Journal of BioTechnology. All rights reserved.