Synthesis and antitumor activity of leinamycin derivatives: Modifications of C-8 hydroxy and C-9 keto groups

A series of leinamycin derivatives were synthesized and evaluated for antitumor activity. Modifications at C-8 and C-9 positions revealed a broad structure-activity relationship in vitro and some derivatives showed potent antiproliferative activity against HeLa S3 cells.