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| 1 | Efficient Syntheses of Permethylated Derivatives of Neolamellarin A,a Pyrrolic Marine Natural Product显示文摘The pyrrole-derived alkaloids with marine origin, especially their permethyl derivatives, have unique structures and promising biological activities. Marine natural product neolamellarins are a collection of lamellarin-like phenolic pyrrole compounds, which can inhibit hypoxia-induced HIF-1 activation. Many pyrrole-derived lamellarin-like alkaloids show potent MDR reversing activity. In this study, five permethylated derivatives of neolamellarin A were synthesized with their MDR reversing activity studied in order to identify new MDR reversal agents. A convergent strategy was adopted to synthesize the permethylated derivatives of neolamellarin A. Pyrrole was first converted into a corresponding N-trisisopropylsilyl(TIPS)-substituted derivative, then through iodination afforded 3,4-diiodinated pyrrole compound. The key intermediate, 3,4-disubstituent-1H-pyrrole, was obtained through desilylation of 3,4-disubstituent-1-TIPS pyrrole, which was prepared from 3,4-diiodinated pyrrole derivative and aryl boronic acid ester through Suzuki cross-coupling reaction between them. Then, the intermediate, 3,4-disubstituent-1H-pyrrole, reacted with fresh phenylacetyl chloride under n-Bu Li/THF condition afforded the target compounds. Finally, we obtained five novel pyrrolic compounds, permethylated derivatives of neolamellarin A 16a-e, in 30%–37% yield through five step reactions. The bioactivity testing of these compounds are in process. | YIN Ruijuan JIANG Long WAN Shengbiao JIANG Tao | 2015 | Journal of Ocean University of China2015，14，2： | 2 |
| 2 | SURFACE REACTION,HYDROGEN DIFFUSIVITY AND ENVIRONMENTAL EMBRITTLEMENT OF INTERMETALLIC COMPOUNDS Ni_3Al AND Fe_3Al显示文摘SURFACEREACTION,HYDROGENDIFFUSIVITYANDENVIRONMENTALEMBRITTLEMENTOFINTERMETALLICCOMPOUNDSNi_3AlANDFe_3AlWANXiaojing;ZHUJiahong;... | WAN Xiaojing ZHU Jiahong HUANG Shengbiao(Shanghai University. Shanghai 200072, China) | 1995 | Acta Metallurgica Sinica(English Letters)1995，8，Z1： | 1 |
| 3 | Total Synthesis of Marine Cyclic Enol-Phosphotriester Salinipostin Compounds显示文摘Due to their structural diversity and variety of biological activities, marine natural products have been the subject of extensive study. These compounds, especially phospholipid polycyclic aromatic hydrocarbons, have a wide range of pharmacological applications, including embedded DNA and central nervous system, anti-tumor, anti-virus, anti-parasite, anti-bacterial, and antithrombotic effects. Unfortunately, the insufficient drug sources have limited the development of these compounds. In this study, we isolated salinpostin compounds from a fermentation solution of marine-derived Salinospora sp., which has a common bicyclic enol-phosphotriester core framework, as well as potent and selective antimalarial activities against P. falciparum with EC_(50)=50 nmolL^(-1). The chemical synthesis of these compounds in greater quantities is necessary for their use in bioactivity studies. Thus we explored a short route with high yields and mild reaction conditions, which can generate combinatorial libraries for drug discovery and lead optimization. We developed a new total synthesis method for six cyclic enol-phosphotriester salinipotin compounds and their diastereomers. For the total synthesis of cyclipostin P, we prepared cyclic enol-phosphotriester salinipostin compounds in 10 steps from a readily accessible starting material, 1,3-dihydroxyacetone, and obtained an overall yield of 1.29%. We fully characterized these compounds by proton nuclear magnetic resonance(~1H-NMR), carbon-13 NMR(^(13)C-NMR), and high-resolution mass spectrometry(HRMS) analyses, and found they coincide absolutely with the same compounds reported previously. | ZHAO Mingliang WEI Xianfeng LIU Xuemeng DONG Xueyang YU Rilei WAN Shengbiao JIANG Tao | 2018 | Journal of Ocean University of China2018，17，3： | 0 |
| 4 | Dextran-DTPA-Gd兔大腿移植瘤腘窝淋巴转移间质磁共振淋巴造影的研究(英文)显示文摘Objective: The aim of the study was to investigate the developing situation of the interstitial magnetic resonance(MR) lymphoid contrast agent Dextran-DTPA-Gd through the rabbit popliteal fossa lymph node metastasis from thigh VX2 transplanted tumor injection to show targeting enhanced metastatic lymph nodes and lymphatics. Methods: VX2 tumor was transplanted to the right hind limb quadriceps of 12 healthy New Zealand rabbits and the left side as a contrast. Eight rabbits had homonymy popliteal lymph node metastasis after 1 month through 3.0 GE MRI and they were later injected with lymphatic targeting contrast agent Dextran-DTPA-Gd 0.4 mL(3.96 × 10–3 mol/L) through bilateral hindlimb toe web respectively. Enhanced MR images were obtained with interval 10 min, 15 min, 20 min, 25 min, 30 min, 35 min, 40 min, 45 min, 50 min, 55 min, 60 min, 2 h, 4 h, and 24 h. The signal intensities before and after enhancing were measured to calculate the enhancing rates(E%) of popliteal lymph node and the popliteal lymph node signal intensity-time curves were drawn to observe the development of cancer metastasis lymph nodes and lymphatics and to compare the differences of interval sides. Results: Ten minutes after injected into the rabbit's bilateral hindlimb toe web, we could see hind lymphatic and popliteal lymph nodes were strengthened significantly and evenly without blood vessels developing. The signal reached a peak after 35 min with E% to 315%, which decreased to 205% after 4 h and would be undifferentiated with the surrounding tissues after 24 h. Statistical analysis was made to popliteal lymph node enhancement rate. It was considered statistically significant as long as P < 0.05. The tumor-side popliteal lymph node manifested as coarse and irregular shape, lymphatic vessels tortuous dilated and lymphatic chain incomplete as a result of tumor infection. Conclusion: Dextran-DTPA-Gd is specific to lymphoid tissue development. It can targeting display regional lymphatic drainage concretion and the morphology of normal and cancer cells metastasis lymph nodes rapidly. | Zhenpeng Zhao Yuanyong Feng Wei Li Shengbiao Wan Tao Jiang Wei Shang | 2014 | The Chinese-German Journal of Clinical Oncology2014，13，5： | 0 |
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