Protein tyrosine kinases have emerged as crucial targets for therapeutic intervention in cancer. More recently, growth factor ligands and their respective receptor tyrosine kinases (RTKs) have been shown to be required for tumor cell growth. This latter aspect includes tumor angiogenesis where the growth of tumors leads to compensatory effects on host cells in the tumor microenvironment leading to the growth of microvessels. The purpose of this review is to focus on synthetic chemical approaches to block RTKs associated with tumor angiogenesis as a means to limit the growth and spread of human tumors.