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Synthesis and Anticancer Activities of Fluorinated Genistein Derivatives

Author: YaoXu
Tutor: ZhengXing
School: Nanhua University
Course: Pharmacology
Keywords: Genistein Derivative Anticancer activity
CLC: R285.5
Type: Master's thesis
Year: 2010
Downloads: 69
Quote: 0
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Abstract


Objective: To enhance the anticancer activity of genistein , we difluoromethylene and genistein group on structural modification , and explore its in vitro anti-cancer activity and structure-activity relationship for the rational design of anti-cancer drugs to provide a theoretical basis . Methods: direct fluorination method difluoromethylene introduce the structure of genistein , and then get a series of alkylated derivatives ; synthesized by the MTT assay genistein derivatives in vitro human colon carcinoma (HT-29) cells, human gastric cancer (SGC-7901) cells and human acute myeloid leukemia (HL-60) cell proliferation inhibition . According to preliminary results of MTT assay , analysis of synthetic genistein derivatives inhibit the HT-29 cells , SGC-7901 cells and HL-60 cell proliferation QSAR . Results: IR, 1H NMR, 13C NMR , mass spectrometry , and elemental fluorine spectral analysis to determine the synthesized a series of genistein derivatives structures and preliminary testing by the MTT assay in vitro for its HT-29 , SGC-7901 and HL-60 three cell lines proliferation . The results showed that genistein fluorinated derivatives on HT-29, SGC-7901 and HL-60 cells with varying degrees of inhibition. Conclusion: get a new series of genistein derivatives , wherein the compound 2c and 2f on HT-29, SGC-7901 and HL-60 cells significantly inhibited the proliferation .

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CLC: > Medicine, health > Chinese Medicine > Of Pharmacy > Pharmacology > Chinese medicine Experimental Pharmacology
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