岩白菜素含氮衍生物的仿生合成

目的以岩白菜素为原料,通过Mannich反应合成出一系列含氮衍生物。方法在甲醇中用岩白菜素与甲醛、不同的仲胺反应。结果得到了三个新的岩白菜素含氮衍生物。     

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??OBJECTIVE To design and synthesize series of quercetin derivatives by introducing allyl or prenyl groups and investigate their antitumor activities in vitro.METHODS Compounds 2, 3, 4, 5, 6, 7 and 8 were synthesized with quercetin as starting material through the etherification reaction.The antitumor activities were evaluated by MTT assay against human lung cells (A549), human breast cancer cells (MDA-MB-231), and human hepatoma cells (HepG2).RESULTS Two allyl-substituted and five prenyl-substituted quercetin derivatives were synthesized. Compounds 4, 5, 6, 7, and 8 were new compounds, and their structures were characterized by ¹H-NMR and ¹³C-NMR. Compounds 6 and 7 exhibited observable anti-proliferative activity. Compound 6 inhibited the growth of A549, MDA-MB-231, and HepG2 cells with IC₅₀ values of 15.23, 16.56, and 12.32 ??mol??L^-1, respectively.Compound 7 restrained the growth of A549 and MDA-MB-231 cells with IC₅₀ values of 8.92 and 2.90 ??mol??L^-1, respectively. CONCLUSION Compounds 6 and 7 synthesized by introducing prenyl groups into quercetin have significant anti-tumor activities, which are worth of further research.     

新型蛇床子素磺酸酯衍生物的合成与抗菌活性研究

目的 为了寻找抗菌候选化合物,对天然产物蛇床子素蛇床子素进行结构改造和生物活性评价.方法 以蛇床子素为原料,经二氧化硒氧化制得中间体1,中间体1经硼氢化钠还原制得中间体2,中间体2再与磺酰氯反应制得目标化合物.采用2倍稀释法对目标物进行体外抗菌活性筛选.结果 合成了16个结构新颖的蛇床子素磺酸酯衍生物,经核磁共振波谱法...     

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??OBJECTIVE To explore the synthesis of novel phenylalanine dipeptide derivatives and their inhibitory effects on tumor cells. METHODS Starting from L-phenylalanine or L-tyrosine, a series of derivatives were synthesized by reaction with chloroacetyl chloride, followed by condensation with L-phenylalaninol or L-phenylalanine methyl ester hydrochloride and nucleophilic substitution reaction with differently substituted phenol.The cell proliferation inhibiting activities of the derivatives were evaluated by thiazolyl blue tetrazolium bromide(MTT)method.RESULTS Some of the target compounds showed certain inhibitory effect for leukemia cell lines K562 and HEL in vitro.Furthermore, the derivatives 3f and 3q had preferably inhibitory effect on K562 cell line prostate cancer PC3 cells in vitro.CONCLUSION Phenylalanine dipeptide derivatives possess good effect on the leukemia and prostate cancer cells and are worth of further research.     

4-氨基-2-三氟甲基喹唑啉衍生物的合成及其体外抗肿瘤活性研究

目的 基于喹唑啉为母核设计发现新型抗肿瘤活性化合物。方法 以邻氨基苯甲酰胺和三氟乙酸酐为起始原料采用缩合、环化、氯代和偶联反应等合成了一系列4-氨基-2-三氟甲基喹唑啉衍生物(5a~5u)。采用四甲基偶氮唑盐(MTT)法评价所得目标化合物对人肺癌细胞A549、人宫颈癌细胞Hela、人白血病细胞K562、人前列腺癌细胞PC-3、人前列腺癌细胞LNCaP这5种肿瘤细胞的体外增殖抑制活性。结果 化合物5c在5 μmol·L^-1时对PC-3肿瘤细胞的抑制率为49.3%,化合物6a对LNCaP和K562、以及6b对PC-3的抑制率超过了50.0%。结论 本实验设计合成的4-氨基-2-三氟甲基喹唑啉类化合物多数具有一定的抗肿瘤活性,特别是4-氨基的N-甲基化产物6a、6b的体外抗肿瘤活性较原型化合物(5n与5u)显著增强,为该类化合物的进一步研究提供参考。     

蝙蝠葛苏林碱衍生物的合成及钙通道阻滞活性的研究

目的：合成蝙蝠葛苏林碱衍生物，寻找优良的钙通道拮抗剂。方法：从蝙蝠葛粗总碱中分离出蝙蝠葛苏林碱，对其酚羟基进行醚化和酯化(或选择性酯化)，并测定其中一些衍生物的钙通道阻滞活性。结果：合成了15个蝙蝠葛苏林碱衍生物，其结构经IR、1^HNMR、MS得到确证；6个衍生物具有一定的钙通道阻滞活性，化合物DSs具有比蝙蝠葛苏林碱、汉防己甲素和异博定更强的钙通道阻滞活性。结论：化合物DSs具有进一步研究的价值。     

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??OBJECTIVE To design and synthesize a series of chlorogenic acid derivatives in order to improve the solubility and lipid-water partition coefficients of chlorogenic acid, and test the bioactiviteies of the target compounds. METHODS The target compounds were synthesized from chlorogenic acid by three-step reactions of hydroxyl protection, acylation, and deprotection. The anti-tumor activities of the compounds were evaluated against two different tumor cell lines by MTT assay, and the DPPH method was used to measure the antioxidant activities of the compounds. RESULTS Eight title compounds were prepared, the structures of the compounds were confirmed by IR and NMR. The MTT assay showed that the compounds exhibited certain antitumor activities and better antioxidant activities, and the activities against A-549 and SGC-7901 tumor cells and the scavenging ratio to DPPH?? were similar to those of chlorogenic acid. CONCLUSION Chlorogenic acid derivatives containing amide group still have antitumor and antioxidant activities.     

丹皮酚异丁酸酯类衍生物的合成及体外降血脂活性研究

目的 研究丹皮酚异丁酸酯类衍生物的合成,寻找比先导化合物丹皮酚降血脂活性更佳的目标化合物.方法 以丹皮酚为原料,碱性条件下与α-溴代异丁酸发生取代反应,再与不同的醇成酯;以HepG2高血脂细胞实验、脂肪酶活性抑制和胆酸盐结合能力实验研究丹皮酚异丁酸酯类衍生物的体外降血脂活性.结果 合成得到6个丹皮酚异丁酸酯类衍生物,化...     

姜黄素衍生物的合成、表征及其体外抗菌活性

目的:研究姜黄素衍生物的合成,表征以及体外抗菌活性。方法:基于姜黄素分子结构含有两个羰基的特点,采用苯胺,4-甲基苯胺,苯肼,2,4-二硝基苯肼以及姜黄素为原料,合成4种稳定的姜黄素Schiff碱衍生物;并对其进行体外抗菌活性测定。结果:合成了4种姜黄素Schiff碱,其中3个未见文献报道,并采用元素分析、紫外、红外以及核磁氢谱对其结构进行表征。4种化合物体外均有抗菌活性。结论:4种姜黄素衍生物都有一定的抗菌活性,其中Schiff碱(4)的抗菌活性较好。     

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??OBJECTIVE To synthesize the derivatives of 8-amino benzofuran[3,2-d]pyrimidine and study their anticancer activities.METHODS The target compounds were synthesized through a series of reactions, and their anticancer activities in vitro were evaluated against COLO205, MCF-7 and K562 cell lines by MTT as assay. RESULTS Nine title compounds were synthesized and confirmed by EI-MS,¹H-NMR and ¹³C-NMR.Compounds 2, 3d and 5c had good inhibition effect against COLO205, MCF-7 and K562 cells.The inhibition rates of compound 5c against COLO205, MCF-7 and K562 cells were 99.58%,78.75% and 98.68% respectively at 10^-4 mol??L^-1. CONCLUSION The anticancer activity of benzofuran[3,2-d] pyrimidine derivatives is worthy of further study.