Both enantiomers R-1 and S-1 of a chiral C60 derivative were synthesized by the reactions of C60 with 1, 1'-bi-2-naphthol bis(azidoacetates) and characterized by FD-MS, fT-IR,1H NMR, 13C NMR, UV-VIS, CD spectra.
A series of novel phosphonoacetic acid derivatives, N-(ethoxycarbonylmethy-ethoxyphosphonyl)-α-amino acid esters and α-amino phosphonates, were synthesized via the reaction of the corresponding phosphonyl chloride ...A series of novel phosphonoacetic acid derivatives, N-(ethoxycarbonylmethy-ethoxyphosphonyl)-α-amino acid esters and α-amino phosphonates, were synthesized via the reaction of the corresponding phosphonyl chloride with amino acid ester hydrochlorides or amino phosphonates in the presence of a base. The preliminary bioassay shows that some compounds show significant anti-viral activity against tobacco mosaic virus (TMV)展开更多
A series of estrone derivatives of amino acids and peptides haze been synthesized by different coupling reagents and the binding affinity of deblocked derivatives to the estrogen receptor of rats uteri have been measu...A series of estrone derivatives of amino acids and peptides haze been synthesized by different coupling reagents and the binding affinity of deblocked derivatives to the estrogen receptor of rats uteri have been measured by a comptetive radiometric bind- ing assay.展开更多
Ammo acid derivatives react with C60 at 110-120℃to form adduct compounds.The products were isolated by column chromatography and were identified by FD-MS,UV-Vis,FT-IR and 13C NMR spectroscopies.
A series of novel Meldrum＇s acid C60 derivatives were prepared in moderate yields from a convenient one-pot reaction of C60, the Meldrum＇s acid derivatives, 12 and 1,8-diazabicyclo-[5,4,0]-undec-7-ene （DBU） in tol...A series of novel Meldrum＇s acid C60 derivatives were prepared in moderate yields from a convenient one-pot reaction of C60, the Meldrum＇s acid derivatives, 12 and 1,8-diazabicyclo-[5,4,0]-undec-7-ene （DBU） in toluene at room temperature under nitrogen atmosphere. All the new compounds were fully characterized by the spectral data and elemental analysis. A carbene intermediate mechanism was proposed for this reaction.展开更多
Objective: To design and synthesize a series of chrysin derivatives and evaluate the antitumor activities with MTT assay, so as to investigate molecular structure-activity relationship with molecular docking.Methods: ...Objective: To design and synthesize a series of chrysin derivatives and evaluate the antitumor activities with MTT assay, so as to investigate molecular structure-activity relationship with molecular docking.Methods: Target products were synthesized with high yield by substitution reaction, hydrolysis reaction,esterification reaction, and saponification reaction in sequence, and activities of all compounds were evaluated with human gastric carcinoma cell lines MGC-803 and human breast carcinoma cell lines MCF-7 through standard MTT assay. Molecular docking results were calculated with Surflex Geom X programme of Sybyl X-2.0 version workstation.Results: 7-O-amino acids chrysin derivatives 6 a–6 l were synthesized and their inhibitory effects were evaluated by comparing the material chrysin with positive control drug 5-fluorouracil(5-FU). Among these derivatives, compound 5 b(IC50= 24.50 ± 2.26 μmol/L), 5 k(IC50= 24.30 ± 2.19 μmol/L), and 6 f(IC50= 24.61 ± 2.01 μmol/L) showed better inhibitory activities against MGC-803 cell lines, and compound 5 g(IC50= 13.15 ± 1.73 μmol/L) and 5 j(IC50= 12.34 ± 1.25 μmol/L) showed better inhibitory activities against MCF-7 cell lines than chrysin and 5-FU. Molecular docking scores showed a credible consistency compared with MTT results.Conclusion: Compounds 5 b, 5 d, 5 g, 5 j, 5 k, and 6 f showed good antiproliferative effects on specific tumor cells, and compound 5 g should be researched further when according to molecular docking.展开更多
熊果酸属于五环三萜类配合物,在自然界中分布广泛,并显示出多种生物活性,如保肝、抗炎、抗病毒、抗癌等多种药理作用.为寻找高效、低毒的熊果酸衍生物,以具有一定生物活性的熊果酸为先导配合物,通过对其C-28位进行结构修饰及C-3位引入...熊果酸属于五环三萜类配合物,在自然界中分布广泛,并显示出多种生物活性,如保肝、抗炎、抗病毒、抗癌等多种药理作用.为寻找高效、低毒的熊果酸衍生物,以具有一定生物活性的熊果酸为先导配合物,通过对其C-28位进行结构修饰及C-3位引入氨基酸,共设计合成了10种未见报道的熊果酸衍生物.目标配合物的结构经1 H NMR、IR和HRMS表征确证,并以其对培养于高铁血红蛋白的金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、耐喹诺酮金黄色葡萄球菌和培养于脑心浸液培养基中的大肠杆菌进行抑菌活性测试.结果表明,经修饰后的熊果酸衍生物对金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、耐喹诺酮金黄色葡萄球菌的抗菌活性较母体配合物有不同程度的提升.展开更多
文摘Both enantiomers R-1 and S-1 of a chiral C60 derivative were synthesized by the reactions of C60 with 1, 1'-bi-2-naphthol bis(azidoacetates) and characterized by FD-MS, fT-IR,1H NMR, 13C NMR, UV-VIS, CD spectra.
文摘A series of novel phosphonoacetic acid derivatives, N-(ethoxycarbonylmethy-ethoxyphosphonyl)-α-amino acid esters and α-amino phosphonates, were synthesized via the reaction of the corresponding phosphonyl chloride with amino acid ester hydrochlorides or amino phosphonates in the presence of a base. The preliminary bioassay shows that some compounds show significant anti-viral activity against tobacco mosaic virus (TMV)
文摘A series of estrone derivatives of amino acids and peptides haze been synthesized by different coupling reagents and the binding affinity of deblocked derivatives to the estrogen receptor of rats uteri have been measured by a comptetive radiometric bind- ing assay.
文摘Ammo acid derivatives react with C60 at 110-120℃to form adduct compounds.The products were isolated by column chromatography and were identified by FD-MS,UV-Vis,FT-IR and 13C NMR spectroscopies.
基金Project supported by the National Natural Science Foundation of China （No. 20532040）.
文摘A series of novel Meldrum＇s acid C60 derivatives were prepared in moderate yields from a convenient one-pot reaction of C60, the Meldrum＇s acid derivatives, 12 and 1,8-diazabicyclo-[5,4,0]-undec-7-ene （DBU） in toluene at room temperature under nitrogen atmosphere. All the new compounds were fully characterized by the spectral data and elemental analysis. A carbene intermediate mechanism was proposed for this reaction.
基金supported by Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study(No.2014-405)Hunan Provincial Department of Education Project(14C1003)
文摘Objective: To design and synthesize a series of chrysin derivatives and evaluate the antitumor activities with MTT assay, so as to investigate molecular structure-activity relationship with molecular docking.Methods: Target products were synthesized with high yield by substitution reaction, hydrolysis reaction,esterification reaction, and saponification reaction in sequence, and activities of all compounds were evaluated with human gastric carcinoma cell lines MGC-803 and human breast carcinoma cell lines MCF-7 through standard MTT assay. Molecular docking results were calculated with Surflex Geom X programme of Sybyl X-2.0 version workstation.Results: 7-O-amino acids chrysin derivatives 6 a–6 l were synthesized and their inhibitory effects were evaluated by comparing the material chrysin with positive control drug 5-fluorouracil(5-FU). Among these derivatives, compound 5 b(IC50= 24.50 ± 2.26 μmol/L), 5 k(IC50= 24.30 ± 2.19 μmol/L), and 6 f(IC50= 24.61 ± 2.01 μmol/L) showed better inhibitory activities against MGC-803 cell lines, and compound 5 g(IC50= 13.15 ± 1.73 μmol/L) and 5 j(IC50= 12.34 ± 1.25 μmol/L) showed better inhibitory activities against MCF-7 cell lines than chrysin and 5-FU. Molecular docking scores showed a credible consistency compared with MTT results.Conclusion: Compounds 5 b, 5 d, 5 g, 5 j, 5 k, and 6 f showed good antiproliferative effects on specific tumor cells, and compound 5 g should be researched further when according to molecular docking.
文摘熊果酸属于五环三萜类配合物,在自然界中分布广泛,并显示出多种生物活性,如保肝、抗炎、抗病毒、抗癌等多种药理作用.为寻找高效、低毒的熊果酸衍生物,以具有一定生物活性的熊果酸为先导配合物,通过对其C-28位进行结构修饰及C-3位引入氨基酸,共设计合成了10种未见报道的熊果酸衍生物.目标配合物的结构经1 H NMR、IR和HRMS表征确证,并以其对培养于高铁血红蛋白的金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、耐喹诺酮金黄色葡萄球菌和培养于脑心浸液培养基中的大肠杆菌进行抑菌活性测试.结果表明,经修饰后的熊果酸衍生物对金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、耐喹诺酮金黄色葡萄球菌的抗菌活性较母体配合物有不同程度的提升.
