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ID: ALA5143534

Journal: Bioorg Med Chem Lett

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

Authors: Liu C, Xu YY, Wen ZH, Dong YH, Liu ZP.

Abstract: 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 μM, respectively, and thus represent promising lead compounds for further development.

CiteXplore: 34838651

DOI: 10.1016/j.bmcl.2021.128474