Abstract
Acetylated betulinic acid (BA) was converted into mono-substituted benzylamides 2–14. Screening in SRB assays showed them as cytotoxic for a variety of different human tumor cell lines. While parent BA was not cytotoxic within the limits of the assay (cut-off 30 μM), the target amides were cytotoxic. Their bioactivity as well as their tumor cell/non-tumor cell selectivity depended on the substitution pattern of the aromatic ring. The most active compound 9 (holding an ortho methoxy substituent) acted mainly by apoptosis.
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