DETERMINATION OF HYDROPHOBICITY OF NONHOMOLOGOUS SERIES OF ANTICANCERDRUGS BY REVERSED-PHASE HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY

The hydrophobicity and specific hydrophobic surface area of 21 commerc ial anticancer drugs were determined by reversed-phase high-performanc e liquid chromatography on an octadecyl-silica column using methanol-w ater mixtures as eluents. Linear correlations were calculated between the log k' values and the methanol concentration of the eluent, the in tercept and slope were considered as the best estimation of the hydrop hobicity and specific hydrophobic surface area. The relationship betwe en retention characteristics and physicochemical parameters of drugs w as evaluated by multivariate mathematical statistical methods, such as principal component analysis followed by two-dimensional non-linear m apping, varimax rotation and by cluster analysis. Anticancer drugs can be well separated by reversed-phase HPLC. Various multivariate mathem atical statistical calculations indicate that the retention of the inv estigated drugs is mainly governed by hydrophobic and steric parameter s. The results suggest that the use of principal component analysis fo llowed by two-dimensional non-linear mapping is superior to cluster an alysis for the evaluation of large retention data matrices.