Abstract:
: A crucial target in drug research is magnifying efficacy and decreasing toxicity. Therefore,
using natural active constituents as precursors will enhance both safety and biological activities.
Despite having many pharmacological activities, caffeic and ferulic acids showed limited clinical
usage due to their poor bioavailability and fast elimination. Therefore, semisynthetic compounds
from these two acids were prepared and screened as anticancer agents. In this study, CA and FA
showed very potent anticancer activity against Caco-2 cells. Consequently, eighteen derivatives
were tested against the same cell line. Four potent candidates were selected for determination of the
selectivity index, where compound 10 revealed a high safety margin. Compound 10 represented a
new scaffold and showed significant cytotoxic activity against Caco-2. Cell-cycle analysis and eval-
uation of apoptosis showed that derivatives 10, 7, 11, 15 and 14 showed the highest proportion of
cells in a late apoptotic stage.
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