Synthesis of Curcuminoids and Evaluation of Their Cytotoxic and Antioxidant Properties

Abstract

Curcumin (<b>1</b>) and ten derivatives (<b>2</b>-<b>11</b>) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC₅₀) values for the more active compounds against HCT-15 and K562 cell lines. Compounds <b>2</b> and <b>10</b> were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that <b>7</b> has potent activity; even stronger than curcumin, α-tocopherol, and quercetin.