Abstract
The metabolites of N-[(trimethylamineboryl)-carbonyl]-L-phenylalanine methyl ester 1
proved to be active in a number of pharmacological screens where the parent had previously demonstrated potent activity. The proposed metabolites demonstrated significant activity as
cytotoxic, hypolipidemic, and anti-inflammatory agents. In cytotoxicity screens several of the
proposed metabolites afforded better activity than the parent compound against the growth of
suspended and solid tumor cell lines. Evaluation of in vivo hypolipidemic activity demonstrated
that the proposed metabolites of 1 were only moderately active and were generally less effective
than the parent compound. Interestingly, L-phenylalanine methyl ester hydrochloride 3, which
contains no boron atom, demonstrated equivalent hypolipidemic activity as the parent at 8
mg/kg/day in