科 研 成 果
获 奖
1. 杨振军,张礼和,张亮仁,金宏威,关注,林桂椿,化学修饰的寡聚核苷酸及其生物学性质研究,2009年教育部高校自然科学奖二等奖。
2. 张礼和,张亮仁,杨振军,闵吉梅,马令台,林桂椿,核酸药物研究,2002年教育部推荐国家科学技术奖二等奖。
3. 张礼和,周德敏,杨振军,合成不同结构的寡核苷酸和锤头状酶性核酸断裂RNA的机理研究,1998年教育部科技进步奖一等奖。
4. 张礼和,马灵台,闵吉梅,于宏武,张亮仁,有生物活性的核苷、核苷酸类化合物研究,1996年国家教委科技进步奖二等奖。
专 利
1. 杨振军,田苗,黄野,陈卓,彭宜红,张礼和,一种应用于siRNA化学修饰的方法及其在抗病毒治疗方面的应用,申请号:201210020028.2。
2. 杨振军,杨先桃,潘德林,关注,郭颖,D,L-鸟嘌啉核苷类似物单磷酸酯及其制备方法和应用,申请号:201210122499.4。
3. 杨振军,武芸,张浩,郭羽佳,陈卓,张礼和,一种siRNA序列化学修饰的方法、产品及其应用,申请号:201110105266.9。
4. 杨振军,戚娜,张亮仁,张礼和,新型环焦磷酸酯类化合物及其制备方法,中国专利,申请号:201010146670.6。
5. 杨振军,邢磊,陈卓,王萌,张礼和,环二鸟苷酸及其类似物和制备方法,中国专利,申请号:201010135002.3。
6. 杨振军,张俊,王卓,黄野,关注,张亮仁,张礼和,异核苷化合物或其亚磷酸胺衍生物及其制备方法和应用,中国专利,申请号:201010146674.4。
7. 杨振军,谢璐佳,郭颖,潘德林,曹颖莉,关注,张礼和,D, L-鸟嘌呤核苷类似物及其制备方法和应用,申请号:201010155136.1。
8. 杨振军,刘洋,王晓锋,张礼和,一种新型肽-链接基-缀合物及其固相合成方法, 中国专利,申请号:200910085088.0。
9. 张礼和,李凌君,杨振军,张亮仁,新型环焦磷酸酯类化合物及其制备方法,中国专利,申请号:200910087498.9。
10. 杨振军,唐晨,潘德林,张礼和,核苷酸磷酯分子及脂质体及其制备方法和应用,中国专利,申请号:200910238737.6。
11. 徐萍,付翌秋,邹晓民,具有蛋白酶体抑制功能的化合物及其制备方法与应用,中国发明专利ZL 2006 1 0012149.7。
12. 雷小平、牛彦等,取代的吡啶类M1受体激动剂、其制备方法及其用途,中国发明专利ZL2005100939492.4。
13. Yangzhi Ling, Androgen synthesis inhibitors, US Patent, 6, 133, 280, 2000。
14. 张礼和等,8-氯腺苷制备抗肿瘤药物,中国发明专利ZL9318707.9, 1998。
15. 张礼和等,具有嘧啶或嘌呤取代基的氢化呋喃衍生物及其制法,中国发明专利ZL94116948.0, 1998。
代表性论文
1. Zhou Y, Ting KY, Lam CMC, Kwong AKY, Xia J, Jin HW, Liu ZM, Zhang LR*, Lee HC and Zhang LH, Design, synthesis and biological evaluation of novel non-covalent inhibitors of human CD38 NADase. ChemMedChem, 2012, 7, 223-228.
2. Fu G, Doerksen RJ*, Xu P*, Assignment of absolute configuration of sulfinyl dilactones: Optical rotations and 1H NMR experiment and DFT calculations. J. Mol. Struct. 2011, 987, 166-173.
3. Chen Z, Kwong AKY, Yang ZJ, Zhang LR*, Lee HC, and Lihe Zhang LH, Studies on the synthesis of nicotinamide nucleoside and nucleotide analogues and their inhibitions towards CD38 NADase. Heterocycles, 2011, 83, 2837-2850.
4. Hu Q, Nie AH, Welsh K, Criso′stomo FRP, Zhu XJ, Li JX, An J, Reed JC, Zhang LR* and Huang ZW*, Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine. Exp. Biol. Med. 2011, 236, 247-251.
5. Dong M, Si YQ, Sun SY, Pu XP, Yang ZJ, Zhang LR, Zhang LH*, Leung FP, Lam CMC, Kwong AKY, Yue JB, Zhou YY, Kriksunov IR, Hao Q, and Lee HC, Design, synthesis and biological characterization of novel inhibitors of CD38. Org. Biomol. Chem. 2011, 9, 3246-3257.
6. Ma YH, Xu B, Fang Y, Yang ZJ, Cui JR, Zhang LR* and Zhang LH, Synthesis and SAR study of novel peptide aldehydes as inhibitors of 20S proteasome. Molecules, 2011, 16, 7551-7564.
7. Ma YH, Qu LL, Liu ZM, Zhang LR*, Yang ZJ, Zhang LH, Synthesis of salinosporamide A and its analogs as 20S proteasome inhibitors and SAR summarization. Curr. Top. Med. Chem. 2011, 11, 2906-2922.
8. Pei L, Xie LJ, Lin Q, Ling XM*, Guan Z, Yang ZJ*, Studies on the adenosine deaminase-catalyzed conversion of adenosine and nucleoside prodrugs by different capillary electrophoresis modes. Analyt. Biochem. 2011, 414, 131-137.
9. Qi N, Jung K, Wang M, Na LX, Yang ZJ*, Zhang LR, Guse AH, Zhang LH*, A novel membrane-permeant cADPR antagonist modified in the pyrophosphate bridge. ChemComm. 2011, 47, 9462-9464.
10. Yan RB, Yuan M, Wu YF, You XF, Ye XS*, Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains. Bioorg. Med. Chem. 2011, 19, 30-40.
11. Niu Y, Wang YH, Zou XM, Yang YM, Ma C, Lü Y, Zhou B, Yuan Y, Du GH and Xu P*. Synthesis and preliminary evaluation of peptidomimetic inhibitors of human β-secretase. Eur. J. Med. Chem. 2010, 45(5), 2089-2094.
12. Wu HM, Yang ZJ, Zhang LR*, and Zhang LH, Concise Synthesis of Novel Acyclic Analogues of cADPR with Ether Chain as Northern Moiety. New J. Chem. 2010, 34, 956-966.
13. Li LJ, Siebrands CC, Yang ZJ, Zhang LR, Guse AH and Zhang LH*, Novel nucleobase-simplified cyclic ADP-ribose analogue: A concise synthesis and Ca2+-mobilizing activity in T-lymphocytes. Org. Biomol. Chem. 2010, 8, 1843-1848.
14. Dong M, Kirchberger T, Huang XC, Yang ZJ, Zhang LR, Guse AH, Zhang LH*, 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. Org. Biomol. Chem. 2010, 8, 4705-4715.
15. Huang XC, Dong M, Liu J, Zhang K, Yang ZJ, Zhang LR* and Zhang LH. Concise syntheses of trifluoromethylated cyclic and acyclic analogues of cADPR. Molecules. 2010, 15, 8689-8701.
16. Li WJ, Cao M, Pei L, Ling XM*, Li BC, Li Q, Yang ZJ*, Study on steady-state kinetics of nucleotide analogues incorporation by non-gel capillary electrophoresis, Electrophoresis. 2010, 31, 507–511.
17. Wu S, Fu YS, Yan RB, Wu YF*, Lei XP, Ye XS*, Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities. Tetrahedron, 2010, 66(19), 3433.
18. Hu L, Zhang LH*, Zhai HB. Syntheses and configuration determination of (+)-Villatamines A and B, two marine natural products. J. Org. Chem. 2009, 74: 7552-7555.
19. Chen WJ, Mou K, Xu B, Ling XM*, Cui JG, Xu P*, Capillary electrophoresis for screening of 20S proteasome inhibitors. Analyt. Biochem. 2009, 394 (1), 62–67.
20. Xu YL, Jin HW, Yang ZJ, Zhang LR, Zhang LH*, Synthesis and biological evaluation of novel neamine-nucleoside conjugates potentially targeting to RNAs. Tetrahedron Lett. 2009, 65, 5228-5239.
21. Xu YL, Jin HW, Yang ZJ, Zhang LR, Wang Q, Li MN, Zhang LH*, Synthesis and evaluation of novel neamine derivatives effectively targeting to RNA. Bioorg. Med. Chem. Lett. 2009, 19, 2103-2106.
22. Ji L, Ma YH, Li J, Zhang LR*, Zhang LH, An efficient synthesis of (R)- and (S)-baclofen via desymmetrization. Tetrahedron Lett. 2009, 50, 6166-6168.
23. Zhang SW, Shi YW, Jin HW, Liu ZM, Zhang LR*, Zhang LH, Covalent complexes of proteasome model with peptide aldehyde inhibitors MG132 and MG101: docking and molecular dynamics study. J. Mol. Model. 2009, 15, 1481-1490.
24. Li Q, Lin GC, Liu L, Yang ZJ*, Zhang LH, Methyl carbonium ion migration during the reaction of 4-chloro-5-methoxyl-3 (2H)-pyridazinone with trifluoroethylation agents. Molecules. 2009, 14, 777-784.
25. Mou K, Xu B, Ma C, Yang XM, Zou XM, Lü Y, Xu P*. Novel CADD-based Peptidyl Vinyl Ester Derivatives as Potential Proteasome Inhibitors. Bioorg. Med. Chem. Lett.. 2008, 18(8), 2198-2202.
26. Fu YQ, Xu B, Zou XM, Ma C, Yang YM, Mou K, Fu G, Lü Y, Xu P*, Design and synthesis of a novel class of furan-based molecules as potential 20S Pproteasome inhibitors. Bioorg. Med. Chem. Lett. 2007, 17(4), 1102-1106.
27. Yang YM, Zou XM, Fu YQ, Mou K, Fu G, Ma C and Xu p*. Synthesis of β-secretase inhibitors containing a hydroxyethylene dipeptide isostere. Syn. Comm. 2007, 37(1), 9-24.
28. Zhang X, Zou XM and Xu P*. Template synthesis of peptidomimetics composed of aspartic acid moiety by ugi four-component condensation reaction. Syn. Comm. 2005, 35(14), 1881-1888.
29. Yan RB, Yan F, Wu YF, Zhang LH, Ye XS, An efficient and improved procedure for preparation of triflyl azide and application in catalytic diazotransfer reation. Tetrahedron Lett, 2005, 46, 8993-8995.
30. Wang Y, Li Q, Cheng SH, Wu YF, Guo DJ, Fan QH, Wang XF, Zhang LH, and Ye XS*, Base-promoted rearrangement of sugar epoxides to unsaturate sugars. Org. Lett. 2005, 7, 5577-5579.
31. Xu P*, Zhang T, Wang WH, Zou XM, Zhang X, Fu YQ, Synthesis of PNA monomers and dimers by ugi reaction, Synthesis (Stuttgart). 2003 (8), 1171-1176.
32. Zhang LR, Zhang YL, Li XH, and Zhang LH, Study on the synthesis and PKA-I binding activities of 5-alkynyl tubercidin analogues. Bioorg. Med.Chem. 2002, 10, 907-912.
33. Huang LJ, Zhang LH, et al., Synthesis and calcium-mobilizing evaluations of N1-glycosyl -substituted stable mimics of cyclic ADP-ribose. J. Med.Chem. 2002, 45, 5340-5352.
34. Chen J, Zhang LR, Min JM, and Zhang LH, 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. Nucleic Acids Res. 2002, 30, 3005-3014.
35. Li XX, Zhang LR, Lu JF, and Zhang LH, et al., Signal peptide mimics conjugated to peptide nucleic acid: a promising solution fro improving cell membrane permeability. Bioconjugate Chem. 2003, 14, 153-157.
36. Chen CP, Li XX, Zhang LR, and Zhang LH, et al., Synthesis of antisense oligonucleotide-peptide conjugate targeting to GLUT-1 in HepG-2 and MCF-7 cells. Bioconjugate Chem. 2002, 23, 525-529.
37. Guan Z, Tian XB, Zhang LR, and Zhang LH, et al., Synthesis and hybridization properties of oligonucleotide consisting of 1’,4’-anhydro-2’,5’-dideoxy- 2’-(thymin-1-yl)-D-altritol. Helv. Chim. Acta. 2002, 85, 1479-1484.
38. Lei Z, Zhang L, Zhang LR, and Zhang LH, et al., Hybrid characteristics of oligonucleotides consisting of isonucleoside 2’,5’-anhydro-3-deoxy-3’- (thymin-1-yl)- D-manitol with different linkage modes. Nucleic Acids Res. 2001, 29, 1470-1475.
代表性著作
1. 雷小平,徐萍主编:药物化学,高等教育出版社,2010年1月。
2. 徐萍主编,药物化学实验教程Experimental Medicinal Chemistry: A Laboratory Textbook,北京大学医学出版社,2010年8月。
3. 徐萍,吴艳芬主编,药物化学 (北京大学医学远程教育系列教材),北京大学医学出版社,2008年3月。
4. 彭师奇,徐萍主编,药物化学原理 (北京大学药学教材),北京大学医学出版社,2006年3月。
5. 仉文升,李安良主编,徐萍副主编,药物化学 (第二版),高等教育出版社 (北京),2005年6月。
6. 仉文升,雷小平主编,药物化学应试指南 (第一版,第二版),北京大学医学出版社,2002年1月,2006年1月。
7. 郑虎主编,徐萍参编,药物化学 (卫生部规划教材,第四版,第五版,第六版),人民卫生出版社 (北京),2000年12月,2003年8月,2007年8月。
8. 徐正主编,徐萍参编,药物化学学习指导与习题集 (第一版,第二版),人民卫生出版社 (北京),2004年4月,2007年8月。
9. 仉文升等,药物化学,高等教育出版社,1999。
10. 张礼和,以核酸为靶的药物研究,科学出版社,1997。
11. 张亮仁等,核酸药物化学,北京医科大学中国协和医科大学联合出版社,1997。
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