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Design and Synthesis of a New Series of Pyrazolopyridine Compounds with Potent Anti-tumor Activities

Author: MengQingYang
Tutor: WangJianWu
School: Shandong University
Course: Organic Chemistry
Keywords: Pyrazolo [ 1,5 - a ] pyridin - Isoxazole ring Synthesis Anti-tumor activity
CLC: TQ463.5
Type: Master's thesis
Year: 2010
Downloads: 253
Quote: 1
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Abstract


In this thesis, including new pyrazolo pyridine design and synthesis of anticancer drugs. Pyrazolo pyridine compounds is a very important class of fused heterocyclic caused widespread research interest in recent years due to its wide range of physiological activity and indole-aza-indole structure similar. These compounds have a good effect in the prevention and treatment of Klinefelter negative and positive bacteria, tumors and cancer, asthma, neurological disorders, osteoporosis and senile dementia. Pyrazolo pyridine derivatives of pyrazole and [3,4-b] pyridine, pyrazolo [1,5-a] pyridine, pyrazolo [4,3-c] pyridin-categories. Undoubtedly the most studied pyrazolo [1,5-a] pyridine compound, its synthesis method mainly includes: Synthesis of pyridine salt of a, by the N-amine; b from 1 - aziridinyl Synthesis; C Synthesis of 5 - Lithium methyl-3 - methyl-pyrazol-1 - carboxylic acid salt and ketene; d by intramolecular condensation reaction synthesis. -Pyrazolo [1,5-a] pyridine compounds of biological activity mainly in: a, as herpes virus inhibitors; as dopamine receptor antibody; c as p38 protein kinase inhibitors; d as adenosine receptor antagonists. But for pyrazolo [1,5-a] pyridine series of compounds in the anti-tumor activity of less Thus, we focus on the pyrazolo [1,5-a] pyridine series of compounds for anti-tumor activity research. After access to a large literature, we found that the isoxazole and isoxazole derivatives are an important class of heterocyclic compounds. They are not only the important synthons and intermediates in organic synthesis, while also having a broad spectrum of pharmacological activity and biological activity. Its major pharmacologically active analgesic, anti-inflammatory, anti-tuberculosis, anti-convulsant, anti-bacterial, anti-nerve excitability and treatment of Alzheimer's disease. The isoxazole compound is a nitrogen-containing heterocyclic compounds of biological activity of a hot, extensive attention by chemists and pharmacologists. Recently, many drug experts will isoxazole ring is introduced into the target compound compounds to improve the anti-tumor activity, and achieved good results. Thus, we would like to the isoxazole ring introduced into the pyrazolo [1,5-a] pyridine ring up in order to improve its anti-tumor activity, we have designed a series of new 2 - phenyl-3 - (5 - (aminomethyl ) isoxazol-3 - yl) -5 - Ethyl-H-pyrazolo [1,5-a] pyridine compounds, and their synthesis. Combined with previous work in our laboratory, we proceed from the acetophenone, 11 (11a-11k) final compounds synthesized after 8-step reaction, all final compounds, as well as an important intermediate structure after the 1HNMR, 13C NMR, IR and LC -MS analysis to verify that the synthetic route is as follows: Then, we will all final compounds as well as an important intermediate of human pancreatic cancer SW-1990 cells, human bladder carcinoma T-24 cells, human breast cancer MCF-7 cells and human lung cancer A-549 test of the cells of the anti-tumor activity. Compound 10, compound 11c, compound 11e on cultured human pancreatic cancer SW-1990 cells, human bladder cancer T-24 cells, human breast cancer MCF-7 cells and human lung carcinoma A-549 cells with certain cell growth inhibition role Compound 11d on human lung cancer A-549 cells and human breast cancer MCF-7 cells having stronger cell growth inhibition having good selectivity.

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