The application of non-combinatorial chemistry to lead discovery

被引:17
作者
Everett, J [1 ]
Gardner, M [1 ]
Pullen, F [1 ]
Smith, GF [1 ]
Snarey, M [1 ]
Terrett, N [1 ]
机构
[1] Pfizer Global R&D, Med Technol, Sandwich CT13 9NJ, Kent, England
关键词
D O I
10.1016/S1359-6446(01)01876-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Non-combinatorial chemistry is a powerful technology for the synthesis of large numbers of compounds, with complete control over the properties of those compounds. We have developed a Library Creation, Registration and Automation system (LiCRA), which harnesses an efficient noncombinatorial chemistry design and synthesis engine, together with high-throughput automated purification. This LiCRA system also operates in a closed loop mode for hit-to-lead optimization, and contains an integrated IT system that controls and facilitates all aspects of the operation from design to registration. Quality has been our watchword, from the quality of compound design through to the quality of the products.
引用
收藏
页码:779 / 785
页数:7
相关论文
共 8 条
[1]   Successful implementation of automation in medicinal chemistry [J].
Coates, WJ ;
Hunter, DJ ;
MacLachlan, WS .
DRUG DISCOVERY TODAY, 2000, 5 (11) :521-527
[2]   Comprehensive survey of combinatorial library synthesis: 1999 [J].
Dolle, RE .
JOURNAL OF COMBINATORIAL CHEMISTRY, 2000, 2 (05) :383-433
[3]   Evaluation of evaporative light-scattering detector for combinatorial library quantitation by reversed phase HPLC [J].
Fang, LL ;
Wan, M ;
Pennacchio, M ;
Pan, JM .
JOURNAL OF COMBINATORIAL CHEMISTRY, 2000, 2 (03) :254-257
[4]   Automated synthesis: new tools for the organic chemist [J].
Hird, NW .
DRUG DISCOVERY TODAY, 1999, 4 (06) :265-274
[5]   RPR's approach to high-speed parallel synthesis for lead generation [J].
Labaudiniere, RF .
DRUG DISCOVERY TODAY, 1998, 3 (11) :511-515
[6]   Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings [J].
Lipinski, CA ;
Lombardo, F ;
Dominy, BW ;
Feeney, PJ .
ADVANCED DRUG DELIVERY REVIEWS, 1997, 23 (1-3) :3-25
[7]   High-throughput purification of compound libraries [J].
Ripka, WC ;
Barker, G ;
Krakover, J .
DRUG DISCOVERY TODAY, 2001, 6 (09) :471-477
[8]   COMBINATORIAL SYNTHESIS - THE DESIGN OF COMPOUND LIBRARIES AND THEIR APPLICATION TO DRUG DISCOVERY [J].
TERRETT, NK ;
GARDNER, M ;
GORDON, DW ;
KOBYLECKI, RJ ;
STEELE, J .
TETRAHEDRON, 1995, 51 (30) :8135-8173