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Home   •   Spotlight  •  rlist1q07j  •  Most Requested Journal Articles 1Q07-Chemistry and Related Science (8)
Most Requested Journal Articles 1Q07-Chemistry and Related Science

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Following is one of the journal articles most requested by researchers using CAS electronic products.



CAS subject entries for this document include: Drug discovery.

CAPLUS COPYRIGHT 2007 ACS on STN

TITLE: In situ click chemistry: a powerful means for lead discovery
AUTHOR(S): Sharpless, K. Barry; Manetsch, Roman
CORPORATE SOURCE: Department of chemistry, University of South Florida, Tampa, FL, 33620-5250, USA
SOURCE: Expert Opinion on Drug Discovery (2006), 1(6), 525-538 CODEN: EODDBX; ISSN: 1746-0441
PUBLISHER: Informa Healthcare
LANGUAGE: English
ABSTRACT:
A review. Combinatorial chem. and parallel synthesis are important and regularly applied tools for lead identification and optimization, although they are often accompanied by challenges related to the efficiency of library synthesis and the purity of the compd. library. In the last decade, novel means of lead discovery approaches have been investigated where the biol. target is actively involved in the synthesis of its own inhibitory compd. These fragment-based approaches, also termed target-guided synthesis (TGS), show great promise in lead discovery applications by combining the synthesis and screening of libraries of low mol. wt. compds. in a single step. Of all the TGS methods, the kinetically controlled variant is the least well known, but it has the potential to emerge as a reliable lead discovery method. The kinetically controlled TGS approach, termed in situ click chem., is discussed in this article.

Updated 5/15/2007 1:16:42 PM
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