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Asymmetric synthesis of 3-butylphthalide using isomannide and isosorbide as chiral auxiliaries

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Chinese Chemical Letters 2007年第11期18卷 1361-1363页

作者： Zhen Li Min yi hua zhang yi Sheng Lai Si Xun Peng Center of Drug Discovery China Pharmaceutical University Nanfing 210009 China

A new approach for asymmetric syntheses of （S） and （R）-3-n-butylphthalide （NBP） is presented. The diastereoselective addition of dibutylzinic to aromatic aldehyde 10 or 11 generated from isomannide- or isosorbid... 详细信息

关键词： Asymmetric synthesis 3-n-Butylphthalide Isomannide Isosorbide

Total Synthesis of (-)-Tetrahydrolipstatin by the Tandem Mukaiyama-aldol Lactonization

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Chinese Chemical Letters 2005年第11期16卷 1448-1450页

作者： Jian yiN Xiao Bo YANG Zai Xin CHEN yi hua zhang Center of Drug Discovery China Pharmaceutical University Nanjing 210009 Jiangsu Yabang Pharm. Res. ＆ Dev. Co. Ltd Nanjing 210004

（-）-Tetrahydrolipstatin 1 was synthesized in three steps and 33.8% overall yield from aldehyde 6 by tandem Mukaiyama-aldol lactonization, which offered a concise, efficient and highly diastereoselective route to this antiobesity drug. We also presented a resolution method for preparation of the crucial intermediate, β- （t-butyldimethylsilyloxy）tetradecanal.

关键词： Tetrahydrolipstatin tandem Mukaiyama-aldol lactonization asymmetric synthesis,(R)-β-hydroxy tetradecanal resolution.

Synthesis and biological evaluation of novel thalidomide analogues as potential anticancer drugs

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Chinese Chemical Letters 2008年第8期19卷 928-930页

作者： Tao Wang yi hua zhang Shan Yu Hui Ji yi Sheng Lai Si Xun Peng a Center of Drug Discovery China Pharmaceutical University Nanjing 210009 China Department of Pharmacology China Pharmaceutical University Nanjing 210009 China

In search of novel anticancer agents, a series of thalidomide analogs （6a-j） were designed and synthesized. Cytotoxicity of these compounds against human hepatoma cells （HepG2） was evaluated by MTT method. Compoun... 详细信息

关键词： Thalidomide 1,3,4-Thiadiazole Anti-tumor activity HepG2

Synthesis and biological evaluation of nitric oxide-releasing sixalkoxyl biphenyl derivatives as anticancer agents

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Chinese Chemical Letters 2008年第2期19卷 149-152页

作者： Xiang Wen Kong yi hua zhang Li Dai Hui Ji yi Sheng Lai Si Xun Peng Center of Drug Discovery China Pharmaceutical University Nanjing 210009 China Department of Pharmacology China Pharmaceutical University Nanjing 210009 China

A series of novel nitric oxide-donating sixalkoxyl biphenyl derivatives （14a-1） were synthesized by coupling furoxan with alkoxyl biphenyl skeleton using amino acids as the spacers, and their cytotoxicity against HepG2 cells in vitro were evaluated by MTT method. It was found that 14c, 14d, 14f, 14i, 14j and 14k showed more potent cytotoxic activities than control 5-fluorouracil. NO release assay of target compounds indicated that the maximum amount of NO released by most active compounds 14c and 14j was about 6 × 10^-2 μmol/L, whereas 14a and 14h with very weak activity only released NO of 1 × 10^-2 μmol/L.

关键词： Nitric oxide-donating sixalkoxyl biphenyl derivatives Furoxan Cytotoxicity

Synthesis and bioactivity of novel phthalimide derivatives

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Chinese Chemical Letters 2008年第1期19卷 26-28页

作者： Tao Wang yi hua zhang Hui Ji Yan Ping Chen Si Xun Peng Center of Drug Discovery China Pharmaceutical University Nanjing 210009 China Department of Pharmacology China Pharmaceutical University Nanjing 210009 China

Novel phthalimide derivatives （4a, 4b and 6a-6e） were designed as hybrids of thalidomide and NO-ASA, and their chemical synthesis and in vitro biological activities were presented. The preliminary results showed that compared to thalidomide 4a and 4b exhibited enhanced activities against ECV304 and HepG2 cells, whereas 6e was more potent against HepG2 cells. 2007 yi hua zhang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

关键词： Thalidomide NO-ASA Antiangiogenic activity Antitumor activity

Synthesis and biological evaluation of glyco-GA compounds as anticancer agents

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Chinese Chemical Letters 2012年第4期23卷 383-386页

作者： Li Qin He Zhong Hu La Mei Yuan Xiao Shan Wang yi hua zhang Center of Drug Discovery China Pharmaceutical UniversityNanjing 210009China Anhui University of Traditional Chinese Medicine Anhui Key Laboratory of Modernized Chinese Material MedicalHefei 230031China

A series of novel glyco-gambogic acid（GA） compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma（HCC） *** compounds showed much better aqueous solubility（0.92- 1.89 mg/mL） than GA（0.013 mg/mL）,and displayed potent inhibition on HCC cells（IC_（50）：0.21-12.23μmol/L） and little affects on non-tumor liver cells（IC_（50）：42.56-86.43μmol/L）,suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.

关键词： Gambogic acid Glyco-GA compounds Anti-hepatocellular carcinoma activity

Synthesis and evaluation of in vitro anticancer activity of novel solasodine derivatives

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Chinese Chemical Letters 2010年第9期21卷 1087-1090页

作者： Xiao Ming Zha Fei Ran zhang Jia Qi Shan yi hua zhang Jun O. Liu Hong Bin Sun Center for Drug Discovery School of Pharmacy China Pharmaceutical UniversiO Nanjing 210009 China Jiangsu Center for Drug Screening China Pharmaceutical University Nanjing 210009 China Department of Pharmacology and Oncology Johns Hopkins University School of Medicine Baltimore MD 21205 USA

Solasodine 11 is a steroidal alkaloid with various biological ***,8 novel solasodine derivatives were synthesized and their effect on prostate cancer cell proliferation was assessed in *** improvement in antiproliferative activity was achieved among some of the synthetic *** particular,19 exhibited the most potent inhibitory effect against the proliferation of PC-3 cell line（IC50= 3.91μmol/L）.

关键词： Solasodine Derivatives In vitro anticancer

Synthesis and biological evaluation of 2,4-diaminopteridine derivatives as nitric oxide synthase inhibitor

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Chinese Chemical Letters 2009年第4期20卷 420-422页

作者： Fei Ma Gang Lu Wei Fen Zhou Qiu Juan Wang yi hua zhang Qi Zheng Yao School of Pharmacy China Pharmaceutical University Nanjing 210009 China

A series of novel 2,4-diamino-pteridines （9a-l） were synthesized and evaluated as inhibitors of inducible nitric oxide synthase （iNOS） in vitro. It was found that 9a, 9d, 9e, 9h, 9i and 91 showed potent inhibitory activities similar to that of methotrexate （MTX）, while the activities of 9b, 9c, 9f, 9g, 9j and 9k are stronger than MTX.

关键词： Nitric oxide Tetrahydrobiopterin Nitric oxide synthase Synthesis Inhibitive activity

Greenhouse Gas Emissions from Northeast China Rice Fields in Fallow Season

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Pedosphere 2007年第5期17卷 630-638页

作者： LIANG Wei SHI yi zhang hua YUE Jin huaNG Guo-Hong Institute of Applied Ecology Chinese Academy of Sciences Shenyang 110016 （China） Graduate School of the Chinese Academy of Sciences Beijing 10005g （China） College of Resources and Environment Huazhong Agricultural University Wuhan 430070 （China）

CH4, N2O and CO2 emissions from northeast Chinese rice fields were measured in the fallow season （November to March） to investigate the effects of freezing-thawing on the emissions. Both CH4 emission from and atmospheric CH4 oxidation by the soil occurred, but the flux was small. During the fallow season, rice fields acted as a minor source of atmospheric CH4, which accounted for about 1% of the CH4 emission during the rice growing period. The field was also a substantial source of atmospheric N20, which ranged between 40 to 77 mg m-2 and eu=counted for 40%-50% of the annual N20 emission. The largest N20 flux was observed in the thawing period during the fallow season. Laboratory incubation tests showed that the largest N20 flux came from the release of N20 trapped in frozen soil. Tillage and rice straw application （either mulched on the soil surface or incorporated in the soil） stimulated the CH4 and CO2 emissions during the fallow season, but only straw application stimulated N2O emission substantially.

关键词： CH4 CO2 freezing-thawing N2O rice field