Abstract
4-Substituted pyrido[1,2-e]purines as anticancer agents have the ability to intercalate with DNA molecules and display improved cytotoxic activities especially towards the resistant cancer cell lines (MCF7R). These compounds were originally synthesized from imidazopyridines via poor yielding synthetic routes. Herein we discuss the development of more efficient strategies towards pyrido[1,2-e]purines. Since pyrido[1,2-e]purines vary mostly by their 4-substituent, we also wanted to develop more efficient strategy where the 4-substituent can be introduced in the last step.