ABSTRACT
This chapter traces the design and construction of original multivalent Copper-conjugated phosphorus dendrimers, their antiproliferative activities against various human cancer cell lines as well as their mode of action via Bax activation. The multivalent Cu-conjugated phosphorus dendrimers represent new and promising first-in-class anti-proliferative agents with an original mechanism of action in nanomedicine. The synthesis and the antitumor activities of the original copper-conjugated phosphorus dendrimers and corresponding monomers. Few anti-cancer small molecules and copper complexes were described as Bax activators. A major contributor for the opening of mitochondrial pores is Bax, a pro-apoptotic member of the Bcl2 protein family. Nanoparticles in general and dendrimers in particular showing potent anti-cancer activity through Bax activation pathway inducing apoptosis tumor cell death. Three different anti-cancer drug waves can be chronologically outlined as follows: conventional chemotherapeutics; anti-cancer drugs based on high molecular-targeting precision; and anticancer drugs targeting cellular multicomponent machineries and effector systems.
