Nace Zidar

TL;DR: Promising recent approaches that have been developed with the aim of circumventing or overcoming MDR are explored, including the pharmaco-modulation of acridine, the use of natural compounds as means to reverse MDR, and the conjugation of anticancer drugs with carriers that target specific tumor-cell components.

TL;DR: The scientific background behind targeting topoisomerase II together with a number of other targets important in cancer therapy are discussed, the present status is reviewed and further options in the field are discussed.

TL;DR: The high-resolution crystal structure of MurD in complex with (R,Z)-2-(3-[{4-([2,4-dioxothiazolidin-5-ylidene]methyl)phenylamino}methyl)benzamido)pentanedioic acid revealed details of the binding mode of the inhibitor within the active site and provides a good foundation for structure-based design of a novel generation ofMurD inhibitors.

TL;DR: A series of hydroxy‐substituted 5‐benzylidenethiazolidin‐4‐ones were synthesized and tested as inhibitors of Mur ligases, and the most potent compound 5 a was active against MurD–F with IC50 values between 2 and 6 μm, making it a promising multitarget inhibitor ofMur ligases.

TL;DR: Stronger antimicrobial activity against S. aureus was observed for compounds bearing the rhodanine ring than those containing other heterocyclic moieties, and both of the compounds 1-11 inhibited the growth of Gram-negative bacteria E. coli or P. aeruginosa.