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Abstract
In the present study, we derivatized several hydroxycinnamic and hydroxybenzoic acids to phenolic amides (PAMs) via one step BOP mediated amide coupling reactions. Fifteen PAMs were synthesized in >40% yields and were screened for their cytotoxic activities against four cancer cell lines: THP-1 (leukaemia), HeLa (cervical), HepG2 (liver), and MCF-7 (breast), in comparison to 5-flurouracil (5-FU). Four amides showed IC50 ranging from 5 to 55 µM against all four cell lines. In contrast, tetradecyl-gallic-amide (13) affected only THP-1 leukaemia cells with IC50 of 3.08 µM. The activities of these compounds support the promise of phenolic amides as anticancer agents.
Graphical Abstract
Disclosure statement
No potential conflict of interest was reported by the authors.
Additional information
Funding
Financial support from the Thailand Research Fund (IRN62W0004) and National Research Council of Thailand (NRCT) and Suranaree University of Technology (SUT), Thailand Science Research and Innovation (TSRI), and the National Science Research and Innovation Fund (NSRF), Grant No. 90464 are gratefully acknowledged.