Synthesis and Biological Activities of Azalamellarins

The synthesis of azalamellarins, a new series of lactam analogues of biologically active lamellarins, was achieved using Cu(I)-mediated and microwave-assisted C-N(amide) bond formation. Seventeen azalamellarins, including N-allylazalamellarins and N-propylazalamellarins chi-D, L-N, and J-dehydro J, were synthesized and evaluated for their cytotoxicity against the cancer cell lines HuCCA-1, A-549, HepG2, and MOLT-3. The results showed that certain azalamellarins exhibited good activities in the micromolar IC(50) value range (IC(50)=the drug concentration that causes 50 % of cell-growth inhibition after 72 h of continuous exposure to the test molecule), comparable to their parent lamellarin analogue.