| Summary: | Cancer is one of the most important causes of death worldwide. Solid tumors represent the great majority of cancers (>90%) and the chemotherapeutic agents used for their treatment are still characterized by variable efficacy and toxicity. Sesquiterpene lactones are a group of naturally occurring compounds that have displayed a diverse range of biological activities including cytotoxic activity. A series of oxygenated and oxy-nitrogenated derivatives (<b>4</b>–<b>15</b>) from the sesquiterpene lactones cumanin (<b>1</b>), helenalin (<b>2</b>), and hymenin (<b>3</b>) were synthesized. The silylated derivatives of helenalin, compounds <b>13</b> and <b>14</b>, were found to be the most active against tumor cell lines, with GI<sub>50</sub> values ranging from 0.15 to 0.59 μM. The ditriazolyl cumanin derivative (<b>11</b>) proved to be more active and selective than cumanin in the tested breast, cervix, lung, and colon tumor cell lines. This compound was the least toxic against splenocytes (CC<sub>50</sub> = 524.1 µM) and exhibited the greatest selectivity on tumor cell lines. This compound showed a GI<sub>50</sub> of 2.3 µM and a SI of 227.9 on WiDr human colon tumor cell lines. Thus, compound <b>11</b> can be considered for further studies and is a candidate for the development of new antitumor agents.
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