Dissertation > Excellent graduate degree dissertation topics show

Design,Synthesis,and Anticancer Activity of Gambogenic Acid Derivatives

Author: HuZhong
Tutor: HeLiQin
School:
Course: Medicinal Chemistry
Keywords: Gambogenic acid Derivative Antitumor Synthesis Biological activity
CLC: R284
Type: Master's thesis
Year: 2013
Downloads: 18
Quote: 0
Read: Download Dissertation

Abstract


Gambogenic acid (GNA) is one of the major active ingredients of gamboge. Theresult has shown that due to its strong anti-tumor activity, broad anti-tumor spectrumand less toxic, the GNA has good curative effect on liver cancer, gastric cancer,nasopharyngeal carcinoma and adenocarcinoma of the lung. Furthermore, because GNAis selective for tumor cells and has less impact on the hematopoietic system and theimmune function in normal animals, it is a natural anti-cancer drug with greatdevelopment prospects. However, the clinical use of GNA was limited due to its poorwater-solubility （<1mg/ml）.As a result, this paper focuses on the structural modification of GNA. On the basisof maintaining the main structure of GNA, we modified the carboxyl group on C-29position by esterification or amidation reaction. Different amines were introduced inorder to obtain target compounds with better water-solubility and higher anti-tumoractivity. This paper consists of four parts:Part one: IntroductionThe paper introduces the research status of gamboge and structure transformation ofgambogic acid.Part two: Design, synthesis of gambogenic acid derivatives1. Technological optimization of GNA preparation2. Design, synthesis of amino esters of GNAWe took gambogenic acid as a leading compound, twelve novel amino estersderivatives of GNA were designed and synthesized, the structures of target compoundswere determined by IR,1H NMR, MS. 3. Design, synthesis of gambogenic acid amidesBase on C-29carboxyl unit of GNA, four novel amino esters derivatives of GNAwere designed and synthesized by structure modification, which introduction ofdifferent nitrogen-containing group, such as morpholine, piperidine, diethylamine andimidazole. The structures of target compounds were determined by IR,1H NMR, MS.Part three: Preliminary study on antitumor activity in vitroTheir antitumor activities were evaluated in vitro by MTT assay.Part four: ConclusionIn conclusion, sixteen target compounds were synthesized by structuremodification. Based on our preliminary results，these compounds have potent antitumoractivity.

Related Dissertations

  1. Studies on the Synthesis and Technology of Dipentaerythritol and Its Derivative,TQ223.164
  2. Video Coding Research Based on Texture Characteristics,TP391.41
  3. Urothermal Synthesis, Structure and Characterization of Functional Coordination Polymers,O631.3
  4. Synthesis and Seperation of 1,1’-binaphthol,O625.3
  5. The Antioxidative Efficient Component Recognition for Curcuma Longa L. Based on the Quality Control Pattern of Constituent Knock-out/Knock-in,R285
  6. Gold-catalyzed Addition Reaction of Sulfonates and Alkynes and Study of Synthesis and Bioactivity of (E)-3-phenyl-substituted Acrylic Acids,R914
  7. Syntheses of Novelbenzopyran Compounds Containing Fluorine and Induced Resistance to TMV,S435.72
  8. Expression of β-Catenin in Pig’s Ovary and the Effect of β-Catenin on Porcine Granulosa Cells Apotosis and Steroidogenesis Related Enzyme,S828
  9. The Problems and Solutions of University’s Ideological and Political Education under Network Environment,G641
  10. The Research on Texture Synthesis Technology from Cloud Theory & Been Evolution Genetic Algorithm,TP391.41
  11. The Study of Protection of Amino Acid and Peptide Bond Synthesis,O629.71
  12. The Oxidation Mechanism and Stability Improved of Conjugated Polyunsaturated Fatty Acids,O621.25
  13. The Small Organic Molecules Targeted Human Telomeric G-quadruplex DNA: Design, Synthesis and Binding Properties,TQ460.1
  14. Antitumor Effect and Expression of the Pro-apoptotic Bcl-2 Family Member N of Elemene in Mice Bearing Hepatocarcinoma H22 Cells-derived Tumor,R285.5
  15. L-4- nitrobenzene alanine amino acid derivatives such as five kinds of biological effects,R96
  16. 1,4 - bis (4 - amino-2 - (trifluoromethyl) phenoxy ) benzene -type Schiff base imide copolymer synthesis and characterization,O631.3
  17. More than enough calcium and magnesium metal ligand complexes Synthesis, Structural Characterization and Antibacterial Activity,O641.4
  18. Schiff base Synthesis, Characterization and Antibacterial Properties,O641.4
  19. Arsenic and antimony chalcogenides Solvothermal Synthesis and Characterization,O641.4
  20. Aldehyde hydrazones and pyrazoline compounds Synthesis and Luminescence Properties,O626
  21. Aza polydentate metal Complexes,O627

CLC: > Medicine, health > Chinese Medicine > Of Pharmacy > Traditional Chinese medicine chemical
© 2012 www.DissertationTopic.Net  Mobile