Synthesis and Antimicrobial and Anticancer Activity of β-Carboline Analogues

Abstract

The β-carboline alkaloids possess a wide diversity of important biochemical effects and pharmacological properties. A series of β-carboline derivatives were synthesized from L-tryptophan through the Pictet-Spengler reaction and oxidation of K2Cr2O7 via sequential one-pot synthesis method. In vitro anti-bacterial, insecticidal, and cytotoxic activities of all synthesized compounds were investigated by the tablet diffusion, leaf disc, and MTT methods, respectively. Some of the compounds(1a, 1b, 1c and 1j) exhibited obvious anti-bacterial effects and some (1-3) had significant cytotoxic activities against tumor cells 3LL, MCF-7, BGC-823 and QGY-7701, with IC50 values of 7.79, 5.75, 3.53 and 4.02 μg/mL, respectively. No insecticidal activity against third stage instar larvae of Mythimnaseparata Walker were observed under the tested concentration.