Development of nature inspired new drug molecules through medicinal chemistry approach has a profound success on drug discovery. Efforts of chemists have succeeded in developing semi-synthetic derivatives to dominate the authentic natural product in terms of drug-likeness properties include increased potency, reduced toxicity and patient compliance. β-carbolines a family of indole-based alkaloids, remained as a privileged scaffold to exhibit anticancer effects through numerous mechanisms. This review inclines the readers towards the ongoing developments (2017-2019) on cytotoxic effects of β-Carboline with an significance on structure based rational drug design, multiparameter lead optimization strategies, relevant SAR studies of this particular framework.