Antitumor Platinum(II) Compounds of a Chiral Diamine with Functionalized Cyclobutane-1,1-Dicarboxylates as Leaving Ligands

摘要

Three novel platinum(II) compounds of bicyclic (R,R)-diamine were obtained and characterized, adopting cyclobutane-1,1-dicarboxylate and 3-hydroxy/3-oxocyclobutane-1,1-dicarboxylate as a leaving group and characterized. According to the IC50 data, the sequence of the cytotoxicity the three compounds is generally 3 > oxaliplatin > 2 > 1 > carboplatin. Among them, compound 3 was much more active than oxaliplatin, against A549 and HepG-2, respectively. Moreover, the compound 3 had lower cytotoxicity than that of oxaliplatin in the HUVEC cell line. Flow cytometry analysis confirmed that compound 3 could make Hep-2 cell dead based on the apoptotic pathway.