The present book discussed development and comparison of the tumor-targeting propensity of ligand decorated dendrimers. Folate-, dextran-, and galactose-anchored PPI dendrimers were synthesized by divergent method, characterized and evaluated for cell cytotoxicity assay. The outcome of project depicted the order of targeting affinity of different ligands under investigation as folate > dextran > galactose. The conclusion is estimated to be of higher scientific value and is assumed to help researcher in choice of targeting ligands.