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We synthesized five novel tryptamine derivatives characterized by the presence of an azelayl chain or of a 1,1,1-trichloroethyl group, in turn connected to another heterocyclic scaffold. The combination of tryptamin-, 1,1,1-trichloroethyl- and 2-aminopyrimidinyl- moieties produced compound <b>9</b> identified as the most active compound in hematological cancer cell lines (IC₅₀ = 0.57–65.32 μM). Moreover, keeping constant the presence of the tryptaminic scaffold and binding it to the azelayl moiety, the compounds maintain biological activity. Compound <b>13</b> is still active against hematological cancer cell lines and shows a selective effect only on HT29 cells (IC₅₀ = 0.006 µM) among solid tumor models. Compound <b>14</b> loses activity on all leukemic lines, while showing a high level of toxicity on all solid tumor lines tested (IC₅₀ 0.0015–0.469 µM).