Design and synthesis of novel heterocylces as potent anticancer and anti-infective agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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| Creator |
Kumar, Ravi
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| Date |
2014-05-12T12:02:05Z
2014-05-12T12:02:05Z 2009 |
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http://hdl.handle.net/123456789/1235
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| Description |
Guide- Dr. P. M. S. Chauhan, PhD Thesis Submitted to JNU, New Delhi in 2009
Cancer, a group of as many as 200 diseases or disorders characterized by uncontrolled division of cells and the ability of these cells to invade other tissues. In the near past cancer has been regarded as a group of diseases affecting the more developed countries but now incidence of various forms of cancer are rapidly rising worldwide. Despite major breakthroughs in the area of medicine in the past century, better understanding of the disease and rationally targeted drugs, successful treatment of cancer still remains a significant challenge. Our goal in this dissertation is to synthesize novel molecules which can selectively inhibit cancer cells proliferation or kill them without affecting normal cells that limits the traditional chemotherapy of cancer. On the other hand, infectious diseases such as leishmaniasis and bacterial infections represent major global health problems of immense proportion and are the leading causes of death in tropical and subtropical regions of the world. Vaccine development against these infectious diseases seems unlikely because of the extreme antigenic variations exhibited by these parasites. Therefore, chemotherapy remains the only treatment option for controlling the infection once acquired. Unfortunately, either resistance has developed to the existing therapeutics or they are toxic to the human host and none of the therapeutic strategy involving these has proven consistently successful. In the light of above facts and the vast biological importance of nitrogen containing heterocycles like triazine, indole, β-carboline, pyrimidine, 2-thiohydantoin, 2-aminoimidazolone and 2-aminoimidazole derivatives inspired us to synthesize these heterocyclic ring systems and their derivatives which may lead to strong drug candidate in the field of cancer and infectious disease like leishmaniasis and bacterial infections. This thesis consists of five chapters. Chapter 1 presents the recent advances in β-carbolines as anticancer and anti-infective agents. This review compiles important developments in natural as well synthetic β-carbolines since January 1996. Among infectious diseases it covers antileishmanial, antimalarial and antifungal β-carbolines. Chapter 2 describes design, synthesis and cytotoxicity evaluation of 1,3,5-triazine and tetrahydro-β-carboline hybrids as anticancer agents.Chapter 3 describes the synthesis of 2-(pyrimidin-2-yl)-1-phenyl-2,3,4,9-tetrahydro-1H-β-carbolines as antileishmanial agents taking inspiration from recently isolated natural product annomontine. Chapter 4 is divided into two parts (a) reviews the literature on marine 2-aminoimidazole, glycociamidine alkaloids and their synthetic analogues as new leads for drug development. While part (b) describes development of highly versatile, protecting group free synthesis of Isonaamine C, it’s analogues and discovery of their antileishmanial and antibacterial potential. Chapter 5 is also divided into two parts, (a) presents a one-pot chemoselective S-alkylation and acetylation of 2- thiohydantoins using the alkyl orthoformate-ZnCl2-Ac2O reagent system. Part (b) describes discovery of SnCl2.2H2O as an efficient reagent for direct and selective oxidative desulfurization of phenylmethylene-2-thiohydantoins to corresponding hydantoins |
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2822284 bytes
application/pdf |
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| Language |
en
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CSIR-CDRI Thesis No. - K-110
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Heterocylces
Anticancer Anti-infective agents |
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| Title |
Design and synthesis of novel heterocylces as potent anticancer and anti-infective agents
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| Type |
Thesis
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