Their role in MDRR was also rationalized. Some physicochemical properties, e.g., the partition coefficient (log P) and the graph index (which in some sense measures the ' complexity ' of a molecule) were also found to be relevant to activity. Possible explanations for these observations are proposed. For example, the CH 2 –CH 2 –N–CH 2 –CH 2 group was found in most of the active compounds, and the activity was further enhanced by the presence of (di)methoxylphenyl groups, whereas the presence of a stable quaternary ammonium salt, a carboxylic, a phenol, or an aniline group was found to be detrimental to activity. Some substructural features related to MDRR activity were identified. To design more effective MDRR agents that are urgently needed for clinical use, a data set of 609 diverse compounds tested for MDRR activity against P388/ADR-resistant cell lines was submitted to the MULTI-CASE computer program for structure-activity analysis. The use of MDR reversal (MDRR) agents is a promising approach to overcome the undesired MDR phenotype. SUMMARY Multidrug resistance (MDR) is one of the major obstacles to long term successful cancer chemotherapy.

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