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Title: Synthesis and Biological Evaluation of Novel Heterocyclic Systems and Synthesis of Dasatinib Through A New Convenient and Efficient Commercial Route
Researcher: Garbapu Suresh
Guide(s): R. Venkata Nadh , N. Srinivasu
University: Vignans Foundation for Science Technology and Research
Completed Date: 2017
Abstract: As per the World Health Organization (WHO) reports, cancer is a fast growing disease in 21st century with an estimation of 13.1 million deaths in 2030 (Wu et al, 2013). The discovery of cancer target potent agents without any side effects is the most challenging issue in cancer research. In view of fast microbial resistance to the existing molecules, discovering the new antibacterial drugs with better pharmacokinetic profile and lesser toxicity has become the main objective in the field of medicinal chemistry. newlineHence, a highly efficient and milder protocol was proposed for the synthesis of hybrid molecules, 2-aminothiazoles bearing 5-methylisoxazoline and pyridine-piperazine scaffolds 52a-e in good yields. The anti-cancer activity of compound 52a was enhanced by electron donating functional group like 2-hydroxyethyl functional substitution on aryl-piperazine heterocyclic systems. This compound was identified as a promising anti-cancer drug lead. Similarly, an alternative new commercial synthetic route was successfully developed to prepare high pure anticancer drug, Dasatinib monohydrate with better yields (68% in Path-A and 61% in Path B). And also, a highly practical method was successfully achieved for the synthesis of novel coumarin-appended isoxazoline derivatives 68a d and 69a d in a good yield via [3 + 2] cycloaddition (1,3-diploar cycloaddition) under mild reaction conditions. The observed highest anti-bacterial activity profile of 68c and 69c suggested that the presence of halogen functional group - bromine had enhanced the activity. newline newline
Pagination: 190
Appears in Departments:Division of Chemistry

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