科研队伍

教育背景:
1986年9月-1990年6月,杭州师范学院(现杭州师范大学),化学系,本科。
1993年9月-1996年6月,华中师范大学,有机合成bobapp官方下载 ,硕士研究生。
1996年9月-2000年1月,bobapp官方下载 ,博士研究生。
工作经历
1990年7月- 1993年7月,浙江省桐庐县窄溪中学,化学教师。
2000年3月- 2002年4月,中国科学院上海有机所,博士后。天然产物全合成、手性药物拆分和不对称合成研究。
2002年5月- 2003年5月,美国肯塔基大学药学院,博士后。烟碱受体拮抗剂的设计与合成;Naltexone前药设计与合成。
2003年6月- 2005年8月,美国堪萨斯大学药物化学系,博士后。以热休克蛋白90 (Hsp90)为靶标的新型抗肿瘤药物设计与合成。
2005年9月- 今,bobapp官方下载 ,历任副研究员、研究员。

1)基于全合成的活性天然产物结构改造与优化;即以全合成为手段、结合药物分子设计的基本原理与方法,对结构比较复杂、但具有显著药物开发前景的天然产物进行有目的的深度结构修饰,以期获得药效更强、毒副作用更小、理化性质更优、更易于实现规模化制备的天然产物类似物。目前该课题主要涉及苯(醌)安莎霉素(如格尔德霉素)和氨基香豆素(如新生霉素)两类天然产物。
2) 以热休克蛋白90 (Heat Shock Protein 90, Hsp90)为作用靶点的新型抗肿瘤药物研究。以课题组前期发现的杂环类小分子Hsp90抑制剂为先导化合物,运用计算机辅助设计方法,进行系统的构效关系探讨和全面的结构优化研究,以期获得具有显著临床应用前景的药物候选物。

1. M. Xu, N. Xue, D. Liu, Y. Zhou, W. Li, Y. Li, X. Chen, X. Yu, 4,5,6,7-Tetrahydro -[1,2,3]triazolo[1,5-a]pyrazine as a new scaffold for heat shock protein 90 inhibitors, Manuscript in preparation.
2. 李永强,严睿,卞传才,张智,刘迪,俞晓明*;格尔德霉素C(11)-C(21)片段的合成;有机化学(Chin. J. Org. Chem.) 2014, 34, 2035-2039.
3.R. Yan, C. Bian, X. Yu, Total synthesis of herbimycin A, Org. Lett. 2014, 16, 3280−3283.
4.C. Bian, R. Yan, X. Yu, Total synthesis of reblastatin: convenient preparation of coupling partners and scaled assembly, Tetrahedron 70, 2982-2991 (2014).
5.D. Liu,X. Yu, L. Huang, Novel Concise Synthesis of (−)-Clausenamide,Chin. J. Chem. 31, 344-8 (2013).
6.L. Zhang, Y. Zhou,X. Yu, Suzuki-Miyaura coupling based enantioselective synthesis of epi-clausemamide and enantiomer of its 3-deoxy analogue.Synlett23, 1217-20 (2012).
7.D. Liu,X. Yu, Ireland-Claisen rearrangement of secondary ally acetate revisited: inevitable C-silylation circumvented by one-pot application of excessive LDA/TMSCl and TBAF. Tetrahed. Lett. 53, 2177-80 (2012).
8.J. Luo,X. Yu, Concise and divergent approach to 3-O-acyl-L-noviose derivatives and their 3-amino bioisosteres: 3-O-benzoyl-L-noviose and N-benzoyl-3-amino-L -noviose. Tetrahed. Lett. 52, 2450 (2011).
9.J. J. Xue,X. M. Yu, Synthesis of 3- and 6-des-phenyl (-)-clausenamide and alternative synthesis of (+)-epi-clausenamide, Chin. Chem. Lett.22, 1261 (2011).
10.J. J. Xue,X. M. Yu, Selective 3- and 6-OH modification of (-)-clausenamide, Chin. Chem. Lett. 22, 761 (2011).
11.Y.-q. He, Y.-q. Li, L. Ma,X.-M. Yu, Synthesis of 4-des-hydroxyl clorobiocin analogues as possible bacterial DNA gyrase B and human Hsp90 inhibitors,J. Chin. Pharm. Sci.20, 218 (2011).
12.Y. He, J. Xue, Y. Zhou, J. Yang,X. Yu, Selective hydroxyl protection of (+)-noviose via improved synthesis,Tetrahed. Lett.50, 2317 (2009).
13.李永强,袁霞,周玉美,罗志刚,陈晓光,俞晓明,热休克蛋白90 (Hsp90) 抑制剂荧光标记探针化合物的设计与合成,中国药物化学杂志 19, 170 (2009).
14.Yu, X. M.; Shen, G.; Neckers, L. M.; Holzbeierlein, J.; Blagg, B. S. J.,Hsp90 Inhibitors Identified from a Library of Novobiocin Analogues. J. Am. Chem. Soc. 127, 12778 (2005). (ACS hot paper)
15.X. M. Yu, Huijong Han, and Brian S. J. Blagg, Synthesis of Mono- and Dihydroxylated Furanoses, Pyranoses, and an Oxepanose for the Preparation of Natural Product Analogue Libraries. J. Org. Chem. 70, 5599 (2005).
16.X. M. Yu, G. Shen, B. S. J. Blagg, Synthesis of (-)-noviose from 2,3-O-Isopropylidene -D-erythronolactol.J. Org. Chem. 69, 7375 (2004).
17.G. Shen,X. M. Yu, B. S. J. Blagg, Synthesis of photolabile novobiocin analogues.Bioorg. & Med. Chem. Lett.14, 5903 (2004). 18.B. WANG,X. M. Yuand G.-q. Lin, The first total synthesis of sphingofungin E and the determination of its stereochemistry.Synlett904 (2001).
19.X. M. Yu, S. Z. Chen and L. Huang, Studies on the total synthesis of hainanolide (VI)-The first access to the lactone function. Chin. Chem. Lett. 11, 295 (2000).
20.T. B. HUNAG,X. M. Yu, L. F. LIU and K. WANG, The synthesis and reaction of heterocyclic thiophosphoryl chlorides with ALCl3 or CF3SO3Ag.Phosphorus, Sulfur and Silicon 156, 9 (2000).
21.X. M. Yu, L. Y. Zhang, S. Z. Chen and L. Huang, Studies on the total synthesis of hainanolide (V)-oxidation of the tricyclic olefines with singlet oxigen.Chin. Chem. Lett.10, 657 (1999).
22.T. B. Huang, K. Wang,X. M. Yuand L. F. Liu, Molecular Structure of 1-diisopropylamino-2-(p-methylphenyl)-3-methylphosph-etane 1-oxide.Jiegou Huaxue17, 329 (1998).
23.W. Q. YANG,X. M. Yu, S. Z. Chen and L. Huang, Studies on the total synthesis of hainanolide (IV)- revising the stereo-chemistry of C2a-H. Chin. Chem. Lett. 8, 1043 (1997).
24.T. B. Huang, L. F. Liu,X. M. Yu, W. Q. Yang, X. H. Qian and J. L. Zhang, Reaction of Shiff Base of Thiohydrazides with P(NR2)3. Phosphorus, Sulfur and Silicon 122, 307 (1997).
25.T. B. Huang, L. F. Liu, W. Q. Yang,X. M. Yu, W. Q. Yang, X. H. Qian and J. L. Zhang,Synthesis of Derivatives of [2,3,4]-thiadiazolo[3,2-c]-1,2,3-trihydro [1,3,5,2]- thia- diazaphosphorins. Phosphorus, Sulfur and Silicon122, 299 (1997).

1.俞晓明,陈晓光,刘迪,吕春婉,李永强,周玉美,马良;三唑并吡嗪(酮)以及异噁唑并哌啶酮类化合物,申请号:201210250715.3 ( 2012)。

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