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Summary
Novelty: New drug resistance agents are provided which sensitize tumour cells to anticancer drugs and/or inhibit the tumour cells' resistance to antitumour drugs. The agents disclosed can be easily prepared synthetically.
Biology: The compounds consist of a binary vinca alkaloid and have a different absolute configuration to vinblastine or vincristine at C-14′ and/or C-16′. The S absolute configuration in the C-16′ position is essential for antitumour activity. The modulators investigated, specifically C-20′-deoxy-C-20′-diethyl vincovaline, are not cytotoxic at up to 25 μM for sensitive cells and 100 μM for resistant cells.