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化学生物学导向的有机合成
  • 项目名称：化学生物学导向的有机合成
  • 项目类别：创新研究群体科学基金
  • 批准号：20621062
  • 申请代码：B0201
  • 项目来源：国家自然科学基金
  • 研究期限：2007-01-01-2009-12-31
  • 项目负责人：马大为
  • 负责人职称：研究员
  • 依托单位：中国科学院上海有机化学研究所
  • 批准年度：2006
中文摘要：

本项目取得了如下进展1) 完成了包括Papuamide B，Salinamide A, Piperazimycins A, TMG-chitotriomycin, Candicanoside A, Lobatoside E和Chlorofusin等7类具有重要生理活性的复杂天然产物的第一次全合成工作。对apratoxin A开展了结构-活性关系及作用机制的研究。2) 完成了具有抗菌活性的Chlorothricin，抗肿瘤作用的Azinomycin B和Saframycin A，以及硫肽类抗生素Nocarthiacin 等的生物合成途径的研究。同时通过代谢途径的遗传修饰，得到了红霉素发酵的高效新菌株，并已经在工业上完成放大。3) 发现了一些分别作用于趋化因子受体、IAP蛋白等重要药靶的选择性调节剂，以及一些细胞自吞噬的抑制剂。其中一个趋化因子受体拮抗剂已经完成了作为治疗爱滋病新药的I期临床研究。4) 发展了利用氨基酸促进的Ullmann反应合成一系列广泛存在于生物活性分子中的含氮含氧杂环的新方法。通过研究新的不对称催化反应和利用串联反应，发展了一些合成生物活性分子的关键骨架的新方法。

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期刊论文
手性恶唑烷－2－硫酮类化合物的高效廉价合成方法
苯并咪唑类杂环化合物及其中间体的合成方法
虎眼万年青OSW－1皂甙的无A、B环的双环类似物、合成方法和用途
犬尿氨酸酶的特异性抑制剂L-邻甲氧基苯甲酰基丙氨酸的合成方法
NMDA受体拮抗剂中间体、合成方法和用途
Exploring the Structural Factors That Affect the Self-Assembly of Hydrogen Bonded Hydrazide Foldames
CuI/4-hydro-L-proline as a more effective catalytic system for coupling of aryl bromides with N-Boc
Synthesis of a tetrasaccharide substrate of heparanase
C环连接有五元杂环的青藤碱衍生物和合成方法
氯丝菌素的生物合成基因簇及应用
Design, synthesis and evaluation of potent, conformationally constrained Smac mimetics
Synthesis of Betavulgaroside III, a representative triterpene seco-glycoside
Effective synthesis of nucleosides with glycosyl trifluoroacetimidates as donors
Xuebin Shao, Zhanting Li, Spectroscopic properties of hydrogen-bond-modulated porphyrin dimer in dif
Biomimetic Total Synthses of Cassiarins A and B
Cholestane glycosides and trihydroxy fatty acids from the rhizomes of Dioscorea septemloba
3－芳基－8－羟基色原酮－7－O－alpha－D－呋喃阿拉伯糖苷化合物及其合成方法和用途
Insights into Conversion of Propargylic Tosylates into Bromoallenes
Elaboration of oxazepine ring system via CuI/L-proline catalyzed intramolecular aryl amination
Expeditious Total Syntheses of Camptothecin and 10-Hydroxycamptothecin
New Analogues of Natural Insect Antifeedant Tonghaosu
Automatic Perception of Organic Molecules Based on Essential Structural Information
Dioseptemlosides A-H: cholestane and spirostane glycosides from the rhizomes of Dioscorea septemloba
Trypanocidal labdane diterpenoids from the seeds of Aframomum aulacocarpos (Zingiberaceae)
Enantioselective organocatalytic Michael addition of malonates to ?,?-unsaturated aldehydes in water
Enantioselective assembly of substituted dihydropyrones via organocatalytic reaction in water media
Antibacterial diterpenoids from Sagittaria pygmaea
Synthesis of Macrocycles from Hydrogen Bonding- Mediated Preorganized Precursors by “Click” Chemistr
Hydrogen Bonding- Mediated Dynamic Covalent Synthesis of Imine-Based Capsules and Formation of Pseud
An efficient route toward 2-amino-beta-D-galacto- and -glucopyranosides via stereoselective Michael-
Current synthesis of triterpene saponins
Polyphyllin D, a potential anti-cancer agent to kill hepatocarcinoma cells with multidrug resistance
Rational Design of Tamiflu Derivatives Targeting at the Open Conformation of Neuraminidase Subtype 1
Enantioselective organocatalytic conjugate addition of aldehydes to α,β-unsaturated thiol esters
Helical Folding of Aromatic Amide-Based Oligomers Induced by 1,3,5-Benzenetricarboxylate Anion in DM
Facile synthesis of 1,4-benzo-diazepin 3-ones from o-bromobenzylamines and amino acids via a cascade
Total synthesis of Candicanoside A, a potent antitumor saponin bearing a rearranged steroid side cha
Synthesis of steroidal saponins bearing an aromatic E ring
The N-dimethylphosphoryl-protected glucosamine trichloro- acetimidate as an effective glycosylation
Synthesis of OSW saponin analogs with modified sugar residues and their antiproliferative activities
Synthesis and In Vitro Antimalarial Activity of Spiro Analogues of Peroxyplakoric Acids
N,N-Dmethylglycine-promoted Ullmann- type coupling reactions of aryl iodides with aliphatic alcohols
Enantioselective total synthesis of 13-O BFA
Design, Synthesis and Evaluation of Tricyclic, Conformationally Constrained Smac Mimetics As Antagon
Intramolecular N(H(((O and N(H(((N Hydrogen Bonding Patterns in N-Benzyl and N-(Pyridin-2-ylmethyl)
Efficient Synthesis of 4-Amido-N5-acetyl-4-deoxy-neuraminic Acid and Its Application to the C-4 Modi
Total synthesis and structural revision of TMG-chitotriomycin, a specific inhibitor of insect and fu
An improved procedure for the nucleosides synthesis with glycosyl trifluoroacetimidates as donors
Efficient and economical access to substituted benzothiazoles: Copper-catalyzed coupling of 2-haloan
Small molecule regulators of autophagy identified by an image-based high throughput screen
Assembly of substituted 3-methyleneisoindolin-1-ones via a CuI/L-proline Catalyzed Domino Reaction P
Assembly of substituted homophthalimides via CuI-catalyzed coupling of 2-bromobenzamides with ?-keto
Intramolecular Six-Membered and Three-Center C(H(((O Hydrogen Bonding in 1,4-Diphenyl- 1,2,3-Triazol
Isoflavone glycosides: synthesis and evaluation as α-glucosidase inhibitor
Carbohydrate chemistry in the total synthesis of saponins
An efficient synthesis of isocoumarins via a Cul catalyzed cascade reaction process
Self-assembly of porphyrin- azulene- porphyrin and porphyrin-azulene conjugates
A Faciel Access to Antiflu Agent Tamiflu/Oseltamivir
Hydrogen bonding-mediated foldamer-bridged zinc porphyrin-C60 dyads. ideal face-to-face orientation
Synthesis of polysubstituted 1,2-dihydroisoquinolines via a CuI-catalyzed arylation- condensation ca
Amino acid promoted Ullmann-type coupling reactions and their applications in organic synthesis
Total synthesis of Lobatoside E, a potent antitumor cyclic triterpene saponin
Gold(I) catalyzed glycosidation of 1,2-anhydrosugars
Dissection of two acyl transfer reactions centered on acyl-S-carrier protein intermediates for incor
Complexation of two non-fully hydrogen bonded aromatic hydrazide heptamers toward n-octyl-(-L-glucop
Synthesis and biological evaluation of 1,3,3,4-tetrasubstituted pyrrolidine CCR5 receptor antagonist
Assembly of substituted 1H-benzimidazoles and 1,3-dihydrobenzimidazol-2-ones via CuI/L-proline catal
I-SOLV: A new surface-based empirical model for computing solvation free energies
Intramolecular six-membered N(H(((Br and N(H(((I hydrogen bonding in aromatic amides
Organocatalytic Michael addition of aldehydes to ?-keto-???-unsaturated esters. An efficient entry t
An Aldol Approach to the Total Synthesis of Pamamycin 621 A
A Novel Small Molecule Regulator of Guanine Nucleotide Exchange Activity of ARF and Golgi Membrane T
Tuning the Acyclic Ether Moiety of Anticancer Agent AA005 with Conformation-Constrained Fragments
Exploration of the correlation between the structure, hemolytic activity, and cytotoxicity of steroi
Synthesis, cytotoxicity, and hemolytic activity of 6’-O-substituted dioscin derivatives
Total synthesis of Candicanoside A, a rearranged cholestane disaccharide, and its 4’’-O-p-methoxyben
Biosynthesis of 3-hydroxy-5-methyl-O- methyltyrosine in the saframycin/ safracin biosynthetic pathwa
Total Synthesis, Assignment of Absolute Chemistry and Structure Revision of Chlorofusin
Polyphyllin D induces mitochondrial fragmentation and acts directly on the mitochondria to induce ap
Synthesis of the A,B-ring-truncated OSW saponin analogs and their antitumor activities
Cholesterol-Appended Aromatic Imine Organogels: A Case Study of the Gelation-Driven Component Select
Five- and Six-Membered N(H(((S Hydrogen Bonding in Aromatic Amides
Computation of Octanol-Water Partition Coefficients by Guiding an Additive Model with Knowledge
Geometrical Preferences of the Hydrogen Bonds on Protein-Ligand Binding Interface Derived from Stati
Molecular modeling of the three-dimensional structure of GLP-1R and its interactions with several ag
Enantioselective Total Synthesis and Absolute Configuration of Megislactone
Construction of Multi-ring Frameworks by Metal-free Cascade Reactions of Stable Isochromenylium Tetr
Transformation of Reactive Isochromenylium Intermediates to Stable Salts and Their Cascade Reactions
Brefeldin A合成新进展
A General and Efficient Approach to Aryl Thiols: Cul-Catalyzed Coupling of Aryl Iodides with Sulfur
Expeditious synthesis of Hippuristanol and congeners with potent antiproliferative activities
Efficient synthesis of Idraparinux, the anticoagulant pentasaccharide
The cytotoxicity of saponins correlates with their cellular internalization
On the Absolute Configuration of Schweinfurthinol
Synthesis of a 1,2,7,8-tetraoxa-spiro[5.5]undecane
Synthesis of 15-demethyl brefeldin A and its 7-epi isomer
外消旋木榄醇甲的简捷合成
青蒿素的生物素标记衍生物的合成
关于茎点霉联烯酸丙的绝对构型
Hydrogen bonded foldamer-bridged biscoumarins： A UV-Vis absorption and fluorescent study of the solvent effect
羰基保护基团的新进展
Brefeldin A全合成研究新进展
Studies Directed toward Synthesis of the Structure Proposed for Stereocalpin A
Synthesis of （-）-Harzialactone A from a Readily Accessible Epoxy Chiral Building Block
Synthesis of an Antitumoral Diarylheptanoid Containing 1,3-Diol Functionality
A Clear-Cut Synthesis of Arteannuin O
马大为的项目
第三届中澳有机化学研讨会
第一届沪台化学学术研讨会
化学生物学导向的有机合成
期刊论文 164
第三届中韩有机化学研讨会
基于蛋白水解酶抑制作用的抗SARS病毒的化合物的合成-活性研究
氨基酸促进的Ullmann类反应及其在合成中的应用
期刊论文 15
具有重要生物活性的生物碱的全合成
具有重要生理活性的两类环肽的合成研究
期刊论文 6
2000年太平洋化学大会
细胞内信号传导系统调节剂的设计和合成
环肽类天然产物的合成和作用机制研究
期刊论文 19
第二届中—韩有机化学会议
细胞自吞噬和细胞凋亡的调控小分子的发现及机理研究
期刊论文 1
2008化学生物学学术研讨会
有机化学
期刊论文 3
第三届中韩有机化学研讨会
生命体系中信息传递的小分子调控
期刊论文 6
参加第二届Tateshina有机化学讨论会
细胞凋亡过程的化学基因学研究
　具有重要生物活性的天然产物的化学合成
期刊论文 26
具有重要生理活性的两类环肽的合成研究
以b-氨基酸衍生物为原料的一些天然产物的合成研究
中美化学生物学青年学者研讨会
第一届中韩双边有机化学学术讨论会
期刊论文 2
化学生物学导向的有机合成
期刊论文 146 会议论文 1
以京尼平为原料的一些萜类天然产物的合成研究
第九届中国多肽会议
第三届世界华人药物化学讨论会