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Title: Synthesis and Anticancer Activity Studies of Some Novel Indole Related Heterocycles
Guide(s): Dalip Kumar
Keywords: Novel Indole, Heterocycles
Physical Sciences,Chemistry,Chemistry Medicinal
University: Birla Institute of Technology and Science
Completed Date: 2018
Abstract: Cancer is one of the prominent causes of death worldwide after heart disease. Identification of potent and selective anticancer drugs with reduced side effects is a serious concern to medicinal chemists. The thesis deals with the design, synthesis and anticancer activity studies of some newlineindole-related heterocycles. The thesis is divided into six chapters. The first chapter briefly highlights the synthesis and chemical properties of indole related heterocycles such as carbazole and and#946;-carboline derivatives. In addition, this chapter includes description about the importance of natural and synthetic carbazole and and#946;-carboline based anticancer agents. newlineThe second chapter is subdivided into two parts dealing with design, synthesis and anticancer activity studies of two different series of novel and#946;-carbolinium bromides. Part A of the chapter reports microwave-assisted rapid and high yielding synthesis of phenacyl-and#946;-carbolinium bromides by N2-quaternization of and#946;-carbolines with 1-aryl-2-bromoethanones in ethanol. The newlinemost potent and#946;-carbolinium bromides were found to display broad spectrum of anticancer activity against all the tested cancer cell lines (IC50 = 3.16-7.93 and#956;M) via apoptosis inducing pathway. Part B of the chapter describes the synthesis and anticancer activity studies of and#946;-carboline-1- newlinechalcones and their bromide salts which led to identify a potent compound with an IC50 value lower than 22.5 and#956;M against all the tested cancer cell lines. Further, preliminary mechanism of action studies indicated that chalcone tethered and#946;-carbolinium bromides triggered apoptosis in newlineMDA-MB-231cells. The third chapter illustrates a significant exploration of molecular iodine and triphenylphosphine combination enabled the facile construction of natural and#946;-carboline skeletons. newlineThe desired products were prepared from easily available indoles and tryptamines by in-situ cyclization of bis(indolyl)ketoamides involving the use of molecular iodine and newlinetriphenylphosphine in DMSO. The present strategy provides an attractive approach to access newline
Pagination: 225
Appears in Departments:Chemistry

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