An efficient method was described for the synthesis of ethyl 9-(2-fluorobenzyl)-1-phenyl-9 H-pyrido[3,4-b]indole-3-carboxylate from the starting material L-tryptophan in good yield. The structure of the synthesised compound was established by H-1-NMR, C-13-NMR, and mass spectrometry, as well as single crystal X-ray diffraction analysis. The synthesised compound was screened for it's in vitro anticancer activity against four human carcinoma cell lines by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results showed that the synthesised compound generated a low IC50 value of 14.2 mu M in human chronic myelogenous leukaemia (CML) K562 cell line, suggesting that this compound has the potential to be developed further for its anticancer activity.