(-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide.