二苯乙烯衍生物的合成与抗癌活性的初步研究

以对硝基甲苯和3,4,5-三甲氧基苯甲醛或3,4-二甲氧基苯甲醛为起始原料,经过缩合、还原和酰化反应,合成了(E)-3,4,5-三甲氧基-4'-乙酰氨基二苯乙烯等4种二苯乙烯衍生物.4种化合物对HepG2和BGC-823两种细胞模型的体外抗癌活性测试结果表明,这些化合物具有良好的抗肿瘤活性且对正常细胞毒性较小.     

Synthesis of Novel Phosphoramide-Tegafur Derivatives Containing Aminopropylsilatrane

Abstract

A series of novel phosphoramide-tegafur derivatives containing γ-aminopropyl silatrane were synthesized via the condensation reactions of phosphoryl dichloride with N¹-(2-furanidyl)-N³-(hydroxyethyl)-5-fluorouracil, followed by condensation with γ-aminopropyl silatrane. The structures of the products were confirmed by ¹H NMR, ³¹P NMR, IR, MS, and elemental analysis. The results of preliminary bioassay showed that the new compounds had an inhibition effect against HCT-8 and Bel-7402 cell lines.     

系列C3α-位芳基取代的四氢吡咯并吲哚骨架衍生物的合成

通过银促进的傅-克反应可以合成系列C3α-位为不同类型芳基取代的四氢吡咯并吲哚骨架的类天然产物.在该合成方法的基础上,发现C3α-位分别为对乙酰氨基苯基取代和甲基吲哚取代的四氢吡咯并吲哚类衍生物3a和3b对多种肿瘤细胞均表现出微摩尔级的活性,是具有重要临床应用前景的药物候选化合物.为了进一步研究该类化合物的成药性及其构效关系,以化合物3a为前体化合物合成了一系列类天然产物(化合物4～17),对其抗肿瘤活性进行了研究,并初步探讨了其构效关系.所合成化合物的结构经1H NMR、13C NMR和HRMS分析确证.本研究为该类化合物的临床前研究奠定了基础.     

Synthesis of oleanolic disaccharide derivatives

Oleanolic acid 1 exists widely in food,medicinal herbs and other plants and possesses many attractive biological activities. Recently,some oleanolic derivatives were reported to have interesting anti-tumor activities.Herein,using association principle of drug design,OA disaccharide 17 was designed and synthesized by coupling a-L-rhamnopyranosyl-(1→2)-a-L-arabinopyranosyl disaccharide moiety,which has proved to be a unique sugar sequence with strongly antitumor activity,and modified OA with a nitrile at C-17.     

Synthesis and Anti-tumor Activity of Novel Glycyrrhetinic Acid Derivatives

Twenty-five derivatives of glycyrrhetinic acid(GA)modified on the A-ring,at C30 and C11 positions were synthesized.Their in vitro cytotoxicity against various cancer cell lines[henrietta lacks strain o...     

拉帕替尼类似物的合成及抗肿瘤活性研究

以N'-(2-氰基-4-碘苯基)-N,N-二甲基甲脒为原料,经过Dimroth重排反应、Suzuki偶联、还原氨化3步反应合成了4种新型的拉帕替尼类似物。借助NMR、IR和HRMS对反应中间体和目标化合物进行结构表征,并采用MTT法在SW480、A549和A431人肿瘤细胞上进行了这些化合物抗肿瘤活性的初步体外评价。结果表明,以上4种化合物均具有明显的抑制肿瘤细胞生长作用,特别是化合物5a对所试肿瘤细胞均表现出良好的生长抑制活性(IC50:5.78~13.38μmol/L),与临床使用的抗肿瘤药物拉帕替尼的活性(IC50:4.80~14.90μmol/L)相当。     

Anticancer Effects of Fusion Protein CAtin on DMBA-induced Carcinogenesis in Buccal Pouch of Chinese Hamster

Aberrant expression ofcarcinoembryonic antigen(CEA)is a common feature for multiple types of cancer,which makes it an attractive target for anticancer therapy.CAtin is a novel dual cancer-specific fusi...     

Synthesis and Anti-tumor Activity of Novel Amide Derivatives of Ursolic Acid

Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3 hydroxyl group show better activities than those with an unsubstituted hydroxyl group.     

VP-16与DNA分子间电子转移的光谱学研究

运用脉冲辐解和圆二色谱技术,对用于治疗肿瘤的依托泊甙(VP-16)与鸟苷酸(GMP)和小牛胸腺DNA分子间电子转移的光谱进行了探讨。用脉冲辐解技术发现了VP-16与GMP之间的电子转移,测得两者之间的反应速率常数为3.16×107 L·mol-1·s-1,并对它们的吸收光谱进行了归属,同时用圆二色谱技术发现了VP-16与小牛胸腺DNA之间相互作用。从而为医学工作者进一步了解和探讨VP-16的抗肿瘤机理提供了直接的理论依据。     

Effect of sonication on different quality parameters of Pinus massoniana pollen

A study was initiated with the objective of evaluating the effects of sonication treatment on important quality parameters of extract of Pinus massoniana pollen. Sonication of extract was done (frequency 20 kHz and various amplitude levels) for 10, 30, 50 min, respectively. As results, total polysaccharide, phenolics and flavonoids significantly increased (P < 0.05). And sonicated P. massoniana pollen displays strong immuno-stimulating activity by increasing proliferations of splenic lymphocytes and subsets of CD4+ T cells (CD3+CD4+), CD8 T cells (CD3+CD8+), and increased Ig secretion. Sonicated P. massoniana pollen also showed anti-tumor function by inhibition of tumor cell proliferation, inhibition of ROS production, up-regulation of GSH/GSSG ration, up-regulating the gene expression of P53, Bax and down-regulating the gene expression of Bcl-2. Findings of the present study suggested the sonication treatment of P. massoniana pollen could improve the quality and bioactivity of P. massoniana pollen, indicating that sonication is effective in processing of pollen and could be a potential process in tumor prevention and treatment.