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The original work of the present book consists of three research projects: The first project entitled: Application of Mannich and Michael reactions in synthesis of pyridopyrimido[2,1-b][1,3,5]thiadiazinones and pyridopyrimido[2,1-b][ 1,3] thiazinones as anticancer agents.The second project entitled: Synthesis of pyridotriazolopyrimidines as antitumor agents. The third project entitled: Synthesis of Novel Thiadiazole and Pyrazoline Derivatives Bearing pyrido[2,3-d]pyrimidinone Moiety. The mechanism of formation of the synthesized compounds was discussed and the assigned structure was established via microanalysis and spectral data (IR, 1HNMR and Mass). In addition, the antitumor activities of the synthesized compounds were investigated and the results revealed that these compounds exhibited promising activities a gainst HepG-2 and MCF-7 cancer cell lines.