Date of Original Version
Biomedical and Pharmaceutical Sciences
A series of synthetic aporphine derivatives structurally related to domesticine and nantenine (ring A, N6 and ring C truncated analogs), was evaluated in MTS cytotoxicity assays against the human colon cancer cell lines, HCT-116 and Caco-2. In general, the C1 position of ring A is tolerant of alkoxy substituents as well as a benzoyl ester functionality. Other modifications evaluated resulted in a decrease in cytotoxic activity. The most potent compounds identified had IC50 values in the range 23–38 μM, comparable to the known cytotoxic agent, etoposide.
Ponnala, S., Chaudhary, S., González-Sarrias, A., Seeram, N. P., & Harding, W. W. (2011). Cytotoxicity of aporphines in human colon cancer cell lines HCT-116 and Caco-2: An SAR study. Bioorganic & Medicinal Chemistry Letters, 21(15), 4462-4464. doi: 10.1016/j.bmcl.2011.06.005
Available at: https://doi.org/10.1016/j.bmcl.2011.06.005
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