LR-2(4-phenyl-3,4-dihydro-indeno[2â,1â]pyramidine-2(1H)- thione; Leni Ritmaleni 2), which designed and assumed to have biologically activity as anticancer, has been successfully synthesized by using the Biginelli reaction. This research was aimed to investigate the effect of benzaldehyde excess in the synthesis of LR-2 and to evaluate the cytotoxic activity of LR-2against HeLa cancer cell lines. The synthesis was done by reacting benzaldehyde, 2-indanone and together with thiourea at one time as said as one pot reaction synthetic methodology and the reaction was acid catalysed. The mole equivalent of benzaldehyde was in excess compare to others. The effect of benzaldehyde in excess is the higher the mole of benzaldehyde, the lower the yield of LR-2. The cytotoxicity of LR-2 was done by using MTT method and the LC50 was 268.15 μM.Key words : LR-2, benzaldehyde, cytotoxic, HeLaÂ
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