Synthesis of aristolactam analogues and evaluation of their antitumor activity

A series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines. Naturally occurring aristolactams, such as aristolactam BII (cepharanone B), aristolactam BIII, aristolactam FI (piperolactam A), N-methyl piperolactam A, and sauristolactam showed moderate antitumor activities in selected cell lines. However, several synthetic aristolactam derivatives exhibited potent antitumor activities against a broad array of cancer cell lines with GI50 values in the submicromolar range.

Graphical abstractA series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines. Compound 34 exhibited potent antitumor activities against a broad array of cancer cell lines with GI50 values in the subnanomolar range.Figure optionsDownload full-size imageDownload as PowerPoint slide