共查询到19条相似文献,搜索用时 109 毫秒
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以DMSO为溶剂,5-氟脲嘧啶(5-Fu)为修饰物,对去甲斑蝥素(2)酸酐环部分进行结构修饰,合成了一个新型的去甲斑蝥素羧酸衍生物(3),其结构经1H NMR和IR表征。采用L9(34)正交试验考察了原料比,反应温度,反应时间及溶剂用量对反应的影响。结果表明,在最佳反应条件[2 0.5 mmol,n(2)∶n(5-Fu)=1.2,于140℃反应6 h,DMSO用量15 mL]下制备的3收率为78.2%。采用MTT法研究了体外3对人肝癌细胞HepG2的抑制活性。结果表明,3在用药量为250μmol·L-1时对HepG2的抑制率为89.5%,其IC50为232.4μmol·L-1。 相似文献
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以顺-二碘-二环戊胺合铂(Ⅱ)为起始原料,经聚合反应和胺化反应制得顺式-二碘-异丙胺-环戊胺合铂(Ⅱ)(2);2分别与氯化钾,1,1-环丁基二羧酸钾和一水合草酸钾反应,合成了3个新型的铂配合物:顺式-二氯-异丙胺-环戊胺合铂(Ⅱ)(1a,收率36.6%),顺式-1,1-环丁基二羧酸-异丙胺-环戊胺合铂(Ⅱ)(1b,收率43.6%)和顺式-草酸-异丙胺-环戊胺合铂(Ⅱ)(1c,收率28.1%),其结构经1H NMR,IR,ESI-MS和元素分析表征。采用MTT法测定了1a~1c对肝癌(SMMC-7721),肺癌(A-549),乳腺癌(MCF-7)和结肠癌(SW480)的体外抑制活性。结果表明,1a~1c对部分癌细胞的IC50值小于40μm,具有一定的体外肿瘤生长抑制活性。 相似文献
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以白杨素(1)为起始原料,与溴代羧酸乙酯经取代反应制得中间体7-O-乙氧羰基烷基白杨素(3a~3d);3a~3d经水解反应合成了7-O-羧烷基化的白杨素衍生物(4a~4d),其中4b~4d为新化合物,其结构经1H NMR,13C NMR,IR和ESI-MS表征。初步的体外抗癌活性实验结果表明,3和4对人肝癌细胞Hep G2和人胃癌细胞MGC-803具有一定的抗癌活性,且大多数化合物的抗癌活性比母体化合物1强,其中6-(5-羟基-2-苯基-4H-苯并吡喃酮-7-氧)己酸(4d,IC504.04μmol·L-1)对MGC-803细胞的活性抑制作用强于阳性药物DDP(IC504.40μmol·L-1)。 相似文献
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Jade Dussart-Gautheret Julia Deschamp Thibaut Legigan Maelle Monteil Evelyne Migianu-Griffoni Marc Lecouvey 《Molecules (Basel, Switzerland)》2021,26(24)
This paper reports on the synthesis of new hydroxymethylene-(phosphinyl)phosphonates (HMPPs). A methodology has been developed to propose an optimized one-pot procedure without any intermediate purifications. Various aliphatic and (hetero)aromatic HMPPs were synthesized in good to excellent yields (53–98%) and the influence of electron withdrawing/donating group substitution on aromatic substrates was studied. In addition, the one-pot synthesis of HMPP was monitored by 31P NMR spectroscopy, allowing effective control of the end of the reaction and identification of all phosphorylated intermediate species, which enabled us to propose a reaction mechanism. Optimized experimental conditions were applied to the preparation of biological relevant aminoalkyl-HMPPs. A preliminary study of the complexation to hydroxyapatite (bone matrix) was carried out in order to verify its lower affinity towards bone compared to bisphosphonate molecules. Moreover, in vitro anti-tumor activity study revealed encouraging antiproliferative activities on three human cancer cell lines (breast, pancreas and lung). 相似文献
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In this study, a novel low molecular weight of acetylaminoglucan (AGA) was obtained and its antitumor activity on H22 tumor-bearing mice was investigated. The results of UV, HPLC and FT-IR showed that AGA present high purity with low molecular weight of 2.76 × 103 Da. Animal experiments showed that AGA could inhibit the proliferation of tumor cells in H22 tumor-bearing mice by protecting the immune organs, enhancing the phagocytosis ability of macrophages, killing activity of NK cells and proliferation capacity of lymphocytes, improving the levels of cytokines in vivo and regulating the distribution of lymphocyte subsets, and the tumor inhibition rate reached to 52.74% (50 mg/kg). Cell cycle determination further indicated that AGA could induce apoptosis of tumor cells and arrests it in S phase. These results will provide a data basis for the potential application of AGA in pharmaceutical industry. 相似文献
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L-Proline has been used as an organocatalyst for an efficient synthesis of 1,8-dioxo-octahydroxanthenes by treatment of aldehydes (aromatic, heteroaromatic, and aliphatic) with 5,5-dimethyl-1,3-cyclohexanedione. Three new compounds have been prepared. 相似文献
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为寻找更为有效的抗肿瘤药物,改善汉防己甲素的抗肿瘤活性,本文以汉防己甲素为原料,经过Suzuki反应设计并合成了6个新的双苄基异喹啉类衍生物。新化合物经过质谱(MS)、核磁共振氢谱(~1H NMR)、核磁共振碳谱(~(13)C NMR)等技术手段进行了结构确证。采用细胞计数试剂盒(CCK-8)法初步评价了6个新化合物对人肺癌细胞(A549)和小鼠白血病细胞(P388)的抗肿瘤活性。结果表明,化合物均有不同程度的抗肿瘤活性,其中化合物H1、H4、H6对A549细胞的抗肿瘤活性(IC5010μmol/L)明显优于阳性对照汉防己甲素。 相似文献
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熊果酸衍生物的合成、表征及其对癌细胞的抑制活性 总被引:1,自引:0,他引:1
以熊果酸为母体化合物,对其3-OH和17-COOH进行结构修饰,设计合成了9个熊果酸衍生物,其结构经IR、1H NMR和MS测试技术确证;噻唑蓝(MTT)比色法考察了所合成衍生物对体外人肝癌细胞HepG2培养增殖的抑制作用,结果显示受试衍生物均对细胞增殖有一定抑制作用,且呈剂量依赖性,其中衍生物9的抑制作用最强;衍生物9与细胞作用24 h后,经Hoechst 33342/PI双染色,倒置荧光显微镜下观察,出现细胞凋亡所具有的高蓝色/低红色荧光图;流式细胞术检测细胞周期发现:细胞被阻滞于S期,且阻滞作用随药物浓度的增加而增强。 相似文献
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甲醇中三环己基氢氧化锡分别与呋喃-2-甲酸、2,4,6-三甲基苯甲酸反应,合成了2个三环己基锡芳香羧酸酯Cy3SnO2CC4H3O(1)和Cy3SnO2CC6H2Me3(2)(Cy为环己基)。通过IR、1H和13C NMR、元素分析及X-射线单晶衍射表征结构。1和2均属单斜晶系,配合物1空间群P21,晶体学参数:a=0.823 04(2)nm,b=1.111 19(3)nm,c=1.283 90(3)nm,β=101.090(2)°,Z=2,V=1.152 27(5)nm3,Dc=1.381 g·cm-3,μ(Mo Kα)=1.127 mm-1,F(000)=496,R1=0.052 9,wR2=0.138 7。配合物2空间群P21/c,晶体学参数:a=0.999 62(2)nm,b=1.415 97(2)nm,c=1.973 59(3)nm,β=94.042 0(10)°,Z=4,V=2.786 53(8)nm3,Dc=1.266 g·cm-3,μ(Mo Kα)=0.937 mm-1,F(000)=1 112,R1=0.0540,wR2=0.161 9。配合物(1)和(2)的中心锡原子均为畸变四面体构型。通过分子间氢键作用,配合物(1)形成二维网状结构。试验表明,配合物1和2具有良好的热稳定性,对人癌细胞Colo205、HepG2、MCF-7、Hela、NCI-H460增殖均有较强的抑制作用。 相似文献