The synthesis of new 2+2 metalla-rectangles via coordination driven self-assembly of octahedral Ru(II) based acceptors and amide donors is described. To evaluate their in vitro cytotoxic properties, preliminary biological assays were carried out for various human cancer cell lines, and our results show that the cytotoxicity level of 3 is comparable or even greater in the cases of SK-hep-1 and HCT-15 than that of the reference drug cisplatin.