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化学进展 1999, Vol. 11 Issue (03): 286- 前一篇   后一篇

• 综述与评论 •

化学多样性空间探索与组合药物设计

徐峻   

  1. (Boehringer Ingelheim Pharmaceuticals Inc., 900 Radgebury Road, Ridgefield, CT 06877-0368, USA)
  • 收稿日期:1998-08-01 修回日期:1999-04-01 出版日期:1999-09-24 发布日期:1999-09-24
下载PDF ( 2032 ) 引用
导出 被引次数 ( 17 | 1 )

Chemical Diversity Exploration and Combinatorial Chemistry in Drug Discovery

Xu Jun   

  1. (Boeh ringer Ingelheim Pharm aceuticals Inc. ,900 Ridgebury Road, Ridgefield, CT 06877- 0368, USA)
  • Received:1998-08-01 Revised:1999-04-01 Online:1999-09-24 Published:1999-09-24

本文综述组合化学的最新进展, 内容涵盖组合化学的基本概念、原理、技术, 在药物发现中的应用, 以及组合化学和其他科学技术分枝的关系。最后, 提出了组合化学工程中亟须研究的一些项目, 介绍了开展这些研究所必需的条件, 并给出了解决方案。

关键词： 组合化学, 药物设计, 高速筛选技术, 化学多样性, 微珠编码, 多组分缩合反应, 虚拟组合化学库

The recent progresses of combinatorial chemistry are reviewed. The basic conceptions, principles, techniques, and applications in drug discovery, relations to other sciences and technology are introduced. At the end, combinatorial chemistry research projects, requirements, and possible solutions are proposed.

Key words: combinatorial chemistry, drug design, high through put screening(HTS), chemical diversity, encoding of beads, multiple-component condensation (MCC), virtual combinat rial library

中图分类号: 

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[ 1 ] Stinson S C, C&EN News, 1998, March 16, 42- 46.
[ 2 ] Sweetnam P M , Price C H, Ferkany J W ,in Burger’s Medicinal Chemistry and Drug Discovery (ed.Wolff M E) , Wiley, New York, 1995, , 697- 731.
[ 3 ] Geyson H M , Meloen R H, Barteling S J , Proc. Natl. Acad. Sci. , 1984, 81, 3998- 4002.
[ 4 ] Furka A , Sebestyen M , Dibo G,in Abstract, 14th Congr. Biochem. , Prague, 1988, 47.
[ 5 ] Merrifield R B, J. Am. Chem. Soc. , 1963, 85, 2149- 2154.
[ 6 ] Houghten R A , Proc. Natl. Acad. Sci. , 1985, 82, 5131- 5135.
[ 7 ] Danheiser S L , Genertic Eng. News, 1993, 13 (Nov. 15) , 1.
[ 8 ] Wilson S R,in Combinatorial Chemistry : Synthesisand Application (Eds. Wilson S R, Czarnik A W ) ,JohnWiley & Sons, 1997, 1- 23.
[ 9 ] Borman, C&EN News, 1998, April 6, 47- 67.
[ 10 ] Danielson E, Devenney M , Giaquinta D M et al. , Science, 1998, 279, 837- 839; Nature, 1997,389, 944- 948;http://symyx.com/publicat.html.
[ 11 ] Willett P,in A Practical Guideto Combinatorial Chemistry (eds. Czarnik A W , Dewitt S H) , ACS,Washington DC, 1997, 17- 48.
[ 12 ] http://www.5z.com/divinfo/reviews.html
[ 13 ] Taylor C P, Marks J L , A d vancesin Neurology , 1998, 76, 41- 47.
[ 14 ] An H Y, CumminsL L , Griffey R H, BharadwajR, HalyB D, FraserA S, Wilsonlingardo L , Risen L M , Wyatt J R, Cook P D, J. Amer. Chem. Soc. , 1997, 119, 3696- 3708.
[ 15 ] Backes B J , Ellman J A , Curr. Opin. Chem. Biol. , 1997, 1, 86- 93.
[ 16 ] Baxter A D, Curr. Opin. Chem. Biol. , 1997, 1, 79- 85.
[ 17 ] Gallop M A , Fitch W L , Curr. Opin. Chem. Biol. , 1997, 1, 94- 100.
[ 18 ] Gravert D J , Janda K D, Chem. Rev. , 1997, 97, 489- 510.
[ 19 ] Gravert D J , Janda K D, Curr. Opin. Chem. Biol. , 1997, 1, 107- 113.
[ 20 ] Hermkens P H H, Ottenheijm H C J , Rees D C, Tetrahedron, 1997, 53, 5643- 5678.
[ 21 ] James I W , Mol. Diversity , 1997, 2, 175- 180.
[ 22 ] Kubinyi H, Drug Disc. Today , 1997, 2, 538- 546.
[ 23 ] Kuhlmann J , Inter. Journal of Clinical Pharmacology & Therapeutics, 1997, 35, 541- 552.
[ 24 ] Lam K S, Lebl M , KrchnBk V , Chem. Rev. , 1997, 97, 411- 448.
[ 25 ] Leadlay P F, Curr. Opin. Chem. Biol. , 1997, 1, 162- 168.
[ 26 ] Loo J A , Eur. Mass Spectrom. , 1997, 3, 93- 104.
[ 27 ] Maehr H, Bioorg. Med. Chem. , 1997, 5, 473- 491.
[ 28 ] Maier E, Meier-Ewert S, Bancroft D, Lehrach H, Drug Disc. Today , 1997, 2, 315- 324.
[ 29 ] Merrifield B, Methodsin Enzymology , 1997, 289, 3- 13.
[ 30 ] Nefzi A , Ostresh J M , Houghten R A , Chem. Rev. , 1997, 97, 449- 472.
[ 31 ] Osborne S E, Ellington A D, Chem. Rev. , 1997, 97, 349- 370.
[ 32 ] Pirrung M C, Chem. Rev. , 1997, 97, 473- 488.
[ 33 ] Spaller M R, Burger M T , Fardis M , Bartlett P A , Curr. Opin. Chem. Biol. , 1997, 1, 47- 53.
[ 34 ] Szostak J W , Chem. Rev. , 1997, 97, 347- 348.
[ 35 ] Warr W A , J. Chem. Inform. Comput. Sci. , 1997, 37, 134- 140.
[ 36 ] Armstrong R W , CombsA P, Tempest P A , Brown S D, Keating T A , Account. Chem. Res. , 1996,29, 123- 131.
[ 37 ] Baldwin J J , Henderson I, Med. Res. Rev. , 1996, 16, 391- 405.
[ 38 ] Crowley J I, Rapoport H, Acct. Chem. Res. , 1976, 9, 135- 144.
[ 39 ] Yedida V , Leznoff C C , Can. J. Chem. , 1980, 58, 1144.
[ 40 ] Chen C, Randall L A , Miller R B, Jones D A , Kurth M J , J. Am. Chem. Soc. , 1994, 116, 2661-2662.
[ 41 ] Kurth M J , RandallL A , Chen C, Melander C, Miller R B, J. Org. Chem. , 1994, 59, 5862- 5864.
[ 42 ] Richter L S, Gadek T R, Tetrahedron Lett. , 1994, 35, 4705.
[ 43 ] Schore N E, Najdi S D J J , J. Am. Chem. Soc. , 1990, 112, 441.
[ 44 ] Farrall M J , Frechet J M J , J. Org. Chem. , 1976, 41, 3877- 3882.
[ 45 ] Deshpande M S, Tetrahedron Lett. , 1994, 35, 5613- 5614.
[ 46 ] Frenette R, Friesen R W , Tetrahedron Lett. , 1994, 35, 9177- 9180.
[ 47 ] Backers B J , Ellmann J A , J. Am. Chem. Soc. , 1994, 116, 11171.
[ 48 ] Yu K L , Deshpande M S, Vyas D M , Tetrahedron Lett. , 1994, 35, 89192 8922.
[ 49 ] Hutchins S M , Chapman K T , Tetrahedron Lett. , 1994, 35, 4055- 4058.
[ 50 ] Patek M , Drake B, Lebl M , Tetrahedron Lett. , 1994, 35, 2227- 2230.
[ 51 ] Boyce R, Li G, Nestler P, Suenag T , StillW C, J. Am. Chem. Soc. , 1994, 116, 7955- 7956.
[ 52 ] Chen C, Randall L A , Miller R B, Jones D A , Kurth M J , J. Am. Chem. Soc. , 1994, 116, 2661-2662.
[ 53 ] Lebl M , Krchnak V , Sepetov N F, Seligmann B, Strop P, Felder S, Biopolymers, 1995, 37, 177-198.
[ 54 ] Brenner S, Lerner R A , Proc. Natl. Acad. Sci. , 1992, 89, 5381- 5383.
[ 55 ] Brenner S, Lerner R A , Proc. Natl. Acad. Sci. , 1992, 89, 5381.
[ 56 ] Nielsen J , Brenner S, Janda K D, J. Am. Chem. Soc. , 1993, 115, 9812.
[ 57 ] Kerr J M , Banville S C, Zuckermann R N , J. Am. Chem. Soc. , 1993, 115, 2529.
[ 58 ] Ohlmeyer M H J , Swanson R N , Dillard L W , Reader J C, Asouline G, Kobayashi R, Wigler M ,Still W C, Proc. Natl. Acad. Sci. , 1993, 90, 10922.
[ 59 ] Geysen H M , Chem. Biol. , 1996, 3 (8) , 679.
[ 60 ] Nicolaou K C, Xiao X Y, Parandoosh Z, SenyeiA , Nova M P, Angew. Chem. Int. E d. Engl. , 1995,34, 2289.
[ 61 ] Armstrong R W , Brown S D, Keating T A , Tempest P A ,in Combinatorial Chemistry : Synthesisand Application (eds. Wilson S R, Czarnik A W ) , John Wiley & Sons, 1997, 153- 190.
[ 62 ] Domine D, Devillers,in Scientific Computingand Automation, 1996, 25- 32.
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