【摘要】：目的設(shè)計(jì)合成出的新的藥物配合物修飾Keggin型多酸的復(fù)合物，對(duì)其進(jìn)行結(jié)構(gòu)表征及抗腫瘤活性研究。探索復(fù)合物的合成規(guī)律，研究其構(gòu)效關(guān)系。 方法復(fù)合物的合成采用水熱合成法；通過(guò)X-射線單晶衍射、X-射線粉粉末衍射、元素分析、差熱-熱重和紅外光譜等方法對(duì)晶體進(jìn)行結(jié)構(gòu)表征。利用MTT法研究新型復(fù)合物的體外抗腫瘤活性(SG7901胃癌細(xì)胞株、SMMC7721肝癌細(xì)胞株)。 結(jié)果合成出4個(gè)新型的藥物配合物修飾Keggin型多酸復(fù)合物。體外抗腫瘤實(shí)驗(yàn)顯示，不同結(jié)構(gòu)的復(fù)合物體現(xiàn)出不同程度的抗腫瘤活性和選擇性。最后計(jì)算得到相應(yīng)的IC50值。 結(jié)論本論文選擇喹諾酮類藥物分子作為有機(jī)配體，用不同過(guò)渡金屬離子來(lái)修飾或者橋連多酸，通過(guò)分子自組裝構(gòu)筑了4個(gè)新型的藥物多酸復(fù)合物： [Cu2(Enro)3H2O][SiW12O40]·H2O (1)； {[Cu(Norf)2]}2[SiW12O40](2)； H2[Ni(Enro)2][SiW12O40]·(Enro)2·2H2O (3)； H4[Ni(Enro)2(H2O)2](β-Mo8O26) H2O (4)。 體外抗SGC7901腫瘤細(xì)胞和SMMC7721腫瘤細(xì)胞表明，Keggin型H4SiW12O40母體化合物對(duì)上述兩種腫瘤沒(méi)有抑制活性，通過(guò)金屬藥物配合物修飾后，銅-喹諾酮配合物對(duì)于多酸的抗腫瘤活性影響較小，，而鎳-喹諾酮配合物對(duì)于多酸的抗腫瘤活性影響較大，說(shuō)明金屬離子對(duì)于電子在多酸與金屬配合物的轉(zhuǎn)移起到了關(guān)鍵作用。同樣化合物4的抗腫瘤活性結(jié)果也表現(xiàn)出同樣的效應(yīng)。
[Abstract]:Aim to design and synthesize a novel drug complex modified with Keggin type polyacid complex and to study its structure characterization and antitumor activity. The synthesis rule and structure-activity relationship of the complexes were studied. Methods the complex was synthesized by hydrothermal synthesis and characterized by X-ray single crystal diffraction, X-ray powder diffraction, elemental analysis, DTA-TG and IR spectra. The antitumor activity of the novel complex in vitro (SG7901 gastric cancer cell line and SMMC7721 hepatoma cell line) was studied by MTT assay. Results four novel drug complexes modified Keggin type polyacid complexes were synthesized. Anti-tumor experiments in vitro showed that the complexes with different structures showed different degree of antitumor activity and selectivity. Finally, the corresponding IC _ (50) values are calculated. Conclusion in this paper, quinolones are selected as organic ligands, and different transition metal ions are used to modify or bridge polyacids. Four novel drug polyacid complexes were synthesized by molecular self-assembly: [Cu2 (Enro) 3H2O] [SiW12O40] H2O (1); {[Cu (Norf) 2]} 2 [SiW12O40] (2); H2 [Ni (Enro) 2] [SiW12O40] (Enro) 2 路2H2O (3); H4 [Ni (Enro) 2 (H2O) 2] (尾-Mo8O26) H2O (4). In vitro anti-SGC7901 tumor cells and SMMC7721 tumor cells showed that Keggin-type H4SiW12O40 parent compounds had no inhibitory effect on the above two kinds of tumors. After modified by metal drug complexes, copper-quinolone complexes had little effect on the antitumor activities of polyacids. Nickel-quinolone complexes have a great effect on the antitumor activity of polyacids, indicating that metal ions play a key role in the transfer of electrons between polyacids and metal complexes. The antitumor activity of the same compound 4 showed the same effect.
【學(xué)位授予單位】：佳木斯大學(xué)
【學(xué)位級(jí)別】：碩士
【學(xué)位授予年份】：2014
【分類號(hào)】：R914

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