Recent Insights into β-Carboline Alkaloids with Anticancer Potential

Abstract

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 a significance on structure based rational drug design, multiparameter lead optimization strategies, relevant SAR studies of this particular framework.

One-Pot Reaction Sequence: N-Acylation/Pictet–Spengler Reaction/Intramolecular [4 + 2] Cycloaddition/Aromatization in the Synthesis of β-Carboline Alkaloid Analogues

“…The β-carboline motif, widespread in both alkaloids and artificial compounds, is a key structural element responsible for diverse and remarkable biological activities. − The A,B,C-tricyclic system of β-carboline in natural compounds is frequently fused through the cycle C with various hetero- or carbocycles, including isoindole and isoquinoline moieties (rings D and E in Figure ). − Thus, the synthesis of polycyclic β-carboline derivatives and the search of biologically active substances among them remain the focus of modern organic chemistry. − …”