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The present work is described in five chapters & focusses on Green synthesis of combi-heterocycles such as Thiadiazole, Pyrimidine, Indole, Imidazole,Thiazole, Chromone and morpholine and their anticancer activity, enzyme assays, docking study, ADMEToxicity study.Chapter I Introduction:It deals with the general introduction about heterocylces, Cancer, Fungal and Bacterial diseases. It explains principles of Green Chemistry and the need of Green chemistry.Chapter II: Literature Survey. Chapter III explains need and objective of the study. The chapter IV consists of three sections in which total forty one novel anticancer agents were synthesized using Green protocol. The synthesized novel coupled hybrid compounds have shown excellent to good anticancer activity on the selected cancer cell lines. Chapter V includes synthesis of novel coupled heterocyclic compounds as antimicrobial agents. The chapter V consists of four sections in which total fifty nine novel antimicrobial agents were synthesized using Green protocol and were evaluated for anti fungal and anti bacterial activity, enzyme assays, Molecular docking study, ADME predictions and Toxicity study. Chapter VI: Future Scope.