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Most Requested Journal Articles 4Q04-Chemistry and Related Science

Following is one of the journal articles most requested by researchers using CAS online services.

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CAS indexed 1 chemical substance from this document. CAS subject entries for this document include: Combinatorial chemistry; Combinatorial library; Drug design; and 3 additional concepts.

CAPLUS COPYRIGHT 2005 ACS on STN

TITLE:	The growing impact of click chemistry on drug discovery
AUTHOR(S):	Kolb, Hartmuth C.; Sharpless, K. Barry
CORPORATE SOURCE:	Department of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA
SOURCE:	Drug Discovery Today (2003), 8(24), 1128-1137 CODEN: DDTOFS; ISSN: 1359-6446
PUBLISHER:	Elsevier Science Ltd.
LANGUAGE:	English

ABSTRACT:
A review. Click chem. is a modular approach that uses only the most practical and reliable chem. transformations. Its applications are increasingly found in all aspects of drug discovery, ranging from lead finding through combinatorial chem. and target-templated in situ chem., to proteomics and DNA research, using bioconjugation reactions. The copper-(I)-catalyzed 1,2,3-triazole formation from azides and terminal acetylenes is a particularly powerful linking reaction, due to its high degree of dependability, complete specificity, and the bio-compatibility of the reactants. The triazole products are more than just passive linkers; they readily assoc. with biol. targets, through hydrogen bonding and dipole interactions. Click chem., a modular approach based on highly reliable chem. transformations, is being applied in all aspects of drug discovery, ranging from lead finding to proteomics and DNA research.