A series of fifty-four commercial aldehydes have been synthesized and evaluated for their activity against peripheral blood mononuclear
cells (PBMC) and four human cancer cell lines, exhibiting potent citotoxicity (IC50 ranging from 0.36 to 4.75 μg mL-1
). The structureactivity relationship (SAR) analysis indicated that the number, the positions and the type of substituents attached into the aromatic and
heteroaromatic ring are critical for the biological activity. The aldehydes 24, 26, 48 and 49 displayed a potent citotoxicity activity compared
to the reference drug doxorubicin being, therefore, this discovery important for the rational design of new compounds against cancer.
Key words: cytotoxicity, substituted aldehydes, drugs, SAR, glioblastoma, ovary, colon