Fig. 4.

Compound lipophilicity and hydrocarbon linker asymmetry are associated with changes in biologic activity. The log of the octanol-water partition coefficient [log P (o/w)] for each compound was plotted against (A) cytotoxicity (CC₅₀ value, 2-h exposure) and anti-HIV-1 activity (IC₅₀ value, VII-IIIB) (Table 1) or (B) the VII-IIIB therapeutic index (Table 2). (C) The VII-IIIB therapeutic index for each compound (Table 2) was plotted against its asymmetry value, which is the absolute value of the difference between n₁ and n₂. Trendlines were determined by least squares regression (Microsoft^® Excel). Pearson product moment correlation coefficients (r) are shown.