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第一部分 奋斗历程1

药物化学家张礼和院士3

第二部分 学术贡献7

一、张礼和院士的学术成就及学术思想9

二、张礼和院士的主要学术论文13

1，2，4-三嗪类化合物的研究——Ⅱ.3-甲硫基-5-羟基-6-甲基-1，2，4-三嗪的不正常甲苯磺酰化反应13

羟基含氮杂环化合物的对甲苯磺酰化反应21

Deglyco-bleomycin Degradation of DNA and Formation of a Structurally Unique Fe（Ⅱ）·CO Complex33

Deglycobleomycin：Total Synthesis and Oxygen Transfer Properties of an Active Bleomycin Analogue39

Total Synthesis of Bleomycin43

环状核苷酸的磷酸酯、磷酰胺的合成及其生物活性的研究47

T4 RNA Ligase Mediated Preparation of Novel “Chemically Misacylated” tRNAPheS52

环状核苷酸衍生物的合成61

腺嘌呤核苷的环磷酰化反应68

DNA Strand Scission by Bleomycin：Catalytic Cleavage and Strand Selectivity73

Synthesis of 9-β-D-（Xylofuranosyl） adenine from Adenosine77

Synthesis of（3’-5’），（2’-5’）-linked Di- and Tri-adenylyl Methylphosphonate Analogs80

Evidence for the Rate-Limiting Departure of the 5’-Oxygen in Nonenzymatic and Hammerhead Ribozyme-Catalyzed Reactions86

Ribozyme Mechanism Revisited：Evidence against Direct Coordination of a Mg2＋ Ion with the pro-R Oxygen of the Scissile Phosphate in the Transition State of a Hammerhead Ribozyme-Catalyzed Reaction93

Synthesis of Lactosyl Phosphate Diester Derivatives of Nucleosides97

Explanation by the Double-metal-ion Mechanism of Catalysis for the Differential Metal-ion Effects on the Cleavage Rates of 5’-oxy and 5’-thio Substrates by a Hammerhead Ribozyme101

Stereoselective Synthesis of 4-deo xy-4-nucleobase-2，5-anhydro-L-mannitol Derivatives110

Synthesis of 2-C-（4-aminocarbonyl-2-thiazoyl）-1，4-anhydro-L-xylitols and Their Fluoro Derivatives117

Studies on the Synthesis and Properties of New PNA Analogs Consisting of Land D-Lysine Backbones123

Synthesis of 5-substituted-3-[（2’S，3’S）-3’-hydroxy-2’-hydroxymethyltetrahydrofuran-3’-y1]-1，2，4-oxadiazoles and Their Epimers128

Hybrid Characteristics of O1igonucleotides Consisting of Isonucleoside 2’，5’-anhydro-3’-deo xy-3’-（thymin-1-yl）-D-mannitol with Different Linkage Modes135

Synthesis of Antisense Oligonucleotide-Peptide Conjugate Targeting to GLUT-1 in HepG-2 and MCF-7 Cells142

Syntheses and Calcium-Mobilizing Evaluations of N1-Glycosyl-Subsituted Stable Mimics of Cyclic ADP-Ribose148

Studies on the Synthesis of a G-rich Octaoligoisonucleotide（isoT） 2（isoG）4（isoT）2 by the Phosphotriester Approach and Its Formation of G-quartet Structure168

Signal Peptide Mimics Conjugated to Peptide Nucleic Acid：A Promising Solution for Improving Cell Membrane Permeability181

A Concise Method for the Preparation of Peptide and Arginine-Rich Peptide-Conjugated Antisense Oligonucleotide188

从生物有机化学到化学生物学197

Synthesis and Biological Evaluation of Novel Membrane-Permeant Cyclic ADP-Ribose Mimics：N1-[（5″-O-Phosphorylethoxy）methyl]-5’-phosphorylinosine 5’，5″-Cyclicpyrophosphate （cIDPRE） and 8-Substituted Derivatives205

Properties of Isonucleotide-Incorporated Oligodeoxynucleotides and Inhibition of the Expression of Spike Protein of SARS-CoV218

A Minimal Structural Analogue of Cyclic ADP-ribose——Synthesis and Calcium Release Activity in Mammalian Cells227

Synthesis and Agonist Activity of Cyclic ADP-Ribose Analogues with Substitution of the Northern Ribose by Ether or Alkane Chains239

Structural Insights into the Effect of Isonucleosides on B-DNA Duplexes Using Molecular-dynamics Simulations256

Studies on Aminoisonucleoside Modified siRNAs： Stability and Silencing Activity268

Three-dimensional Structure of HIV-1 VIF Constructed by Comparative Modeling and the Function Characterization Analyzed by Molecular Dynamics Simulation279

Generation of shRNA Pool Library：A Revision of the Biological Technique from the Viewpoint of Chemistry291

A Convenient Preparation of 5-Iodo-1，4-disubstituted-1，2，3-triazole：Multicomponent One-Pot Reaction of Azide and Alkyne Mediated by CuI-NBS295

Chemical Biology in China Takes on Signal Transduction301

Solid-phase Synthesis and Evaluation of TAR RNA Targeted β-carboline-nucleoside Conjugates307

CD38/cADPR/Ca2＋ Pathway Promotes Cell Proliferation and Delays Nerve Growth Factor-induced Differentiation in PC12 Cells318

A Novel Membrane-permeant cADPR Antagonist Modified in the Pyrophosphate Bridge330

Novel Nucleobase-simplified Cyclic ADP-ribose Analogue：A Concise Synthesis and Ca2-mobilizing Activity in T-lymphocytes335

Trifluoromethylated Cyclic-ADP-ribose Mimic：Synthesis of 8-trifluoromethyl-N1-[（5″-O-phosphorylethoxy） methyl]-5’-O-phosphorylinosine-5’，5″-cyclic Pyrophosphate （8-CF3-cIDPRE） and Its Calcium Release Activity in T Cells343

Catalysis-Based Inhibitors of the Calcium Signaling Function of CD38356

A Novel Fluorescent Cell Membrane-permeable Caged Cyclic ADP-ribose Analogue369

Strand Antagonism in RNAi：an Explanation of Differences in Potency between Intracellularly Expressed siRNA and shRNA382

Synthesis and Properties of Novel L-isonucleoside Modified Oligonucleotides and siRNAs392

A Cell Permeable NPE Caged ADP-Ribose for Studying TRPM2406

Studies on CD38 Inhibitors and Their Application to cADPR-Mediated Ca2＋Signaling422

三、主要学术著作438

MEDICINAL CHEMISTRY OF NUCLEIC ACIDS438

化学生物学进展456

以核酸为作用靶的药物研究462

四、张礼和院士学术年表467

张礼和院士论文目录467

张礼和院士主要学术著作目录491

张礼和院士主要奖项目录492

第三部分 治学之道493

锲而不舍 金石可镂——记北医大药学院院长张礼和教授497

攀登药化科学高峰的人——记中科院院士、药物化学家张礼和498

张礼和：平平常常学者心501

张礼和：为祖国药学事业耕耘的人504

张礼和：走在“药学”的路上506

张礼和：院士潜心药物学511

医药科技发展需建长效激励机制——张礼和院士谈“中国药学会科学技术奖”512

用化学方法研究生命过程514

生物医药产业：跟踪创新更实际516

第四部分 大师风范519

科学家的良心与责任——访北京大学药学院张礼和院士521

张礼和：“教学和科研都马虎不得”524

言传身教育桃李——记中国科学院院士、北京大学医学部张礼和教授527

张礼和院士受聘为南开大学杨石先讲座教授531

10人获“北京市人民教师”称号532

张礼和院士获“北京市人民教师”荣誉称号533

2012北京市人民教师奖：张礼和教授主要事迹534

张礼和：惜守良心535

用化学方法研究生命过程的人——张礼和536

北京大学药学院张礼和院士访问沈阳药科大学538

张礼和院士：多给点时间 为青年科学家“减负”539

张礼和院士2012年9月6日在北京市庆祝教师节大会上的发言540

张礼和：院士潜心药物学542

张礼和院士谈创新型人才543

张礼和院士应邀在基因化学与化学基因组合论坛上作报告545

稳扎稳打攻药学，戒骄戒躁求创新——药学院张礼和院士奖学金颁奖仪式暨大学生应具有的学术精神和国际视野讲座546

张礼和院士：医药创新人才的培养547

张礼和院士等四位专家来我校讲学548

北京大学张礼和院士来武汉大学化学与分子科学学院讲学549

张礼和院士来沈阳药科大学作学术报告550

北京大学医学部张礼和院士前来合肥微尺度物质科学国家实验室进行学术交流与访问551

张礼和院士访问武汉大学药学院552

张礼和院士莅临我院 逸仙化学论坛开讲553

第五部分 社会影响555

张礼和：“中国不能没有具有自己知识产权的新药”558

张礼和院士获2011年中国化学会有机合成发展促进奖564

张礼和院士喜获“Nagai-Hisamitsu杰出科学家奖”565

共攀生物医药新高峰——张礼和院士访谈566

张礼和院士赴长春应用化学所作报告567

张礼和院士：我们制造了不少敌人568

张礼和院士访问国家化合物样品库569

张礼和与江雷院士莅临福建物构所参观考察570

北京大学创新药物研究院571

全国科学技术名词审定委员会574

第六部分 人生风采575