Synthesis and biological evaluation of BU-4664L derivatives as potential anticancer agents

BU-4664L is a naturally occurring N-farnesylated dibenzodiazepinone with important biological activities. Herein, we report the synthesis and antitumor evaluation of two series of BU-4664L derivatives bearing different substituent patterns on the dibenzodiazepinone core and with diverse side chains. All of the derivatives displayed micromolar activity against the human prostate cancer PC-3 cells, while lower or no activity against the human lung H460 cells. The most active derivatives were 10a and 16c which exerted antiproliferative activity against PC-3 cells with GI50 values of 5.66 and 5.94 mu M, respectively, and thus represent promising lead compounds for further development.

Automated summary

The study reported the synthesis and evaluation of antitumor activity of two series of BU-4664L derivatives. All derivatives displayed micromolar activity against PC-3 cells, with 10a and 16c showing the most promising antiproliferative activity.