Synthetic Analogues of the Montanine-type Alkaloids with Activity Against Apoptosis-resistant Cancer Cells




Govindaraju, Karthik
Ingels, Aude
Hasan, Md Nabiul
Sun, Dandan
Mathieu, Veronique
Masi, Marco
Evidente, Antonio
Kornienko, Alexander

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In a search of small molecules active against apoptosis-resistant cancer cells, a skeletal rearrangement of alkaloid haemanthamine was utilized to generate a series of compounds possessing the alkaloid montanine ring system. The synthesized compounds were found to inhibit proliferation of cancer cells resistant to apoptosis at micromolar concentrations. Selected compounds were also active against patient-derived glioblastoma cells expressing stem-cell markers. This is the first report describing the preparation of synthetic analogues of the montanine-type alkaloids with antiproliferative activity. The compounds prepared in the current investigation appear to be a useful starting point for the development of agents to fight cancers with apoptosis resistance, and thus, associated with poor prognoses.



apoptosis resistance, montanine, haemanthamine, manthine, antiproliferative activity, Chemistry and Biochemistry


Govindaraju, K., Ingels, A., Hasan, M. N., Sun, D., Mathieu, V., Masi, M., Evidente, A., & Kornienko, A. (2018). Synthetic analogues of the montanine-type alkaloids with activity against apoptosis-resistant cancer cells. Bioorganic and Medicinal Chemistry Letters, 28(4), pp. 589–593.


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