Ferrocenyl and organic novobiocin derivatives: Synthesis and their in vitro biological activity

Abstract A focused series of novobiocin derivatives containing a ferrocene unit together with their corresponding organic novobiocin analogues have been synthesized in modest to good yields. These compounds were screened for biological activity against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) and human breast cancer cell line (HCC38). With the exception of compounds 5c and 5d , the general trend observed is that incorporation of the ferrocene moiety into novobiocin scaffold resulted in compounds 6a – d / 6f showing enhanced activity compared to organic analogues 5a – b and 5e – f .