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 Complex 33
Deglycobleomycin:Total Synthesis and Oxygen Transfer Properties of an Active Bleomycin Analogue 39
Total Synthesis of Bleomycin 43
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” tRNAPheS 52
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 Selectivity 73
Synthesis of 9-β-D-(Xylofuranosyl) adenine from Adenosine 77
Synthesis of(3’-5’),(2’-5’)-linked Di- and Tri-adenylyl Methylphosphonate Analogs 80
Evidence for the Rate-Limiting Departure of the 5’-Oxygen in Nonenzymatic and Hammerhead Ribozyme-Catalyzed Reactions 86
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 Reaction 93
Synthesis of Lactosyl Phosphate Diester Derivatives of Nucleosides 97
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 Ribozyme 101
Stereoselective Synthesis of 4-deo xy-4-nucleobase-2,5-anhydro-L-mannitol Derivatives 110
Synthesis of 2-C-(4-aminocarbonyl-2-thiazoyl)-1,4-anhydro-L-xylitols and Their Fluoro Derivatives 117
Studies on the Synthesis and Properties of New PNA Analogs Consisting of Land D-Lysine Backbones 123
Synthesis of 5-substituted-3-[(2’S,3’S)-3’-hydroxy-2’-hydroxymethyltetrahydrofuran-3’-y1]-1,2,4-oxadiazoles and Their Epimers 128
Hybrid Characteristics of O1igonucleotides Consisting of Isonucleoside 2’,5’-anhydro-3’-deo xy-3’-(thymin-1-yl)-D-mannitol with Different Linkage Modes 135
Synthesis of Antisense Oligonucleotide-Peptide Conjugate Targeting to GLUT-1 in HepG-2 and MCF-7 Cells 142
Syntheses and Calcium-Mobilizing Evaluations of N1-Glycosyl-Subsituted Stable Mimics of Cyclic ADP-Ribose 148
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 Structure 168
Signal Peptide Mimics Conjugated to Peptide Nucleic Acid:A Promising Solution for Improving Cell Membrane Permeability 181
A Concise Method for the Preparation of Peptide and Arginine-Rich Peptide-Conjugated Antisense Oligonucleotide 188
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 Derivatives 205
Properties of Isonucleotide-Incorporated Oligodeoxynucleotides and Inhibition of the Expression of Spike Protein of SARS-CoV 218
A Minimal Structural Analogue of Cyclic ADP-ribose——Synthesis and Calcium Release Activity in Mammalian Cells 227
Synthesis and Agonist Activity of Cyclic ADP-Ribose Analogues with Substitution of the Northern Ribose by Ether or Alkane Chains 239
Structural Insights into the Effect of Isonucleosides on B-DNA Duplexes Using Molecular-dynamics Simulations 256
Studies on Aminoisonucleoside Modified siRNAs: Stability and Silencing Activity 268
Three-dimensional Structure of HIV-1 VIF Constructed by Comparative Modeling and the Function Characterization Analyzed by Molecular Dynamics Simulation 279
Generation of shRNA Pool Library:A Revision of the Biological Technique from the Viewpoint of Chemistry 291
A Convenient Preparation of 5-Iodo-1,4-disubstituted-1,2,3-triazole:Multicomponent One-Pot Reaction of Azide and Alkyne Mediated by CuI-NBS 295
Chemical Biology in China Takes on Signal Transduction 301
Solid-phase Synthesis and Evaluation of TAR RNA Targeted β-carboline-nucleoside Conjugates 307
CD38/cADPR/Ca2+ Pathway Promotes Cell Proliferation and Delays Nerve Growth Factor-induced Differentiation in PC12 Cells 318
A Novel Membrane-permeant cADPR Antagonist Modified in the Pyrophosphate Bridge 330
Novel Nucleobase-simplified Cyclic ADP-ribose Analogue:A Concise Synthesis and Ca2-mobilizing Activity in T-lymphocytes 335
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 Cells 343
Catalysis-Based Inhibitors of the Calcium Signaling Function of CD38 356
A Novel Fluorescent Cell Membrane-permeable Caged Cyclic ADP-ribose Analogue 369
Strand Antagonism in RNAi:an Explanation of Differences in Potency between Intracellularly Expressed siRNA and shRNA 382
Synthesis and Properties of Novel L-isonucleoside Modified Oligonucleotides and siRNAs 392
A Cell Permeable NPE Caged ADP-Ribose for Studying TRPM2 406
Studies on CD38 Inhibitors and Their Application to cADPR-Mediated Ca2+Signaling 422
三、主要学术著作 438
MEDICINAL CHEMISTRY OF NUCLEIC ACIDS 438
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