Literature DB >> 26315392

Discovery of bioactive molecules from CuAAC click-chemistry-based combinatorial libraries.

Xueshun Wang1, Boshi Huang1, Xinyong Liu2, Peng Zhan3.   

Abstract

The rapid assembly and in situ screening of focused combinatorial fragment libraries using CuAAC click chemistry is a highly robust and efficient strategy for establishing SAR and for discovering bioactive molecules. This review outlines the current status of this methodology in drug discovery application. The inherent limitations, challenges and prospects are critically discussed.
Copyright © 2015 Elsevier Ltd. All rights reserved.

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Year:  2015        PMID: 26315392     DOI: 10.1016/j.drudis.2015.08.004

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  20 in total

1.  Evaluating the Contribution of Transition-State Destabilization to Changes in the Residence Time of Triazole-Based InhA Inhibitors.

Authors:  Lauren A Spagnuolo; Sandra Eltschkner; Weixuan Yu; Fereidoon Daryaee; Shabnam Davoodi; Susan E Knudson; Eleanor K H Allen; Jonathan Merino; Annica Pschibul; Ben Moree; Neil Thivalapill; James J Truglio; Joshua Salafsky; Richard A Slayden; Caroline Kisker; Peter J Tonge
Journal:  J Am Chem Soc       Date:  2017-02-22       Impact factor: 15.419

2.  Site-Selective Copper-Catalyzed Azidation of Benzylic C-H Bonds.

Authors:  Sung-Eun Suh; Si-Jie Chen; Mukunda Mandal; Ilia A Guzei; Christopher J Cramer; Shannon S Stahl
Journal:  J Am Chem Soc       Date:  2020-06-23       Impact factor: 15.419

3.  Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.

Authors:  Ye Tian; Zhaoqiang Liu; Jinghan Liu; Boshi Huang; Dongwei Kang; Heng Zhang; Erik De Clercq; Dirk Daelemans; Christophe Pannecouque; Kuo-Hsiung Lee; Chin-Ho Chen; Peng Zhan; Xinyong Liu
Journal:  Eur J Med Chem       Date:  2018-03-23       Impact factor: 6.514

4.  Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors.

Authors:  Gaochan Wu; Yun Gao; Dongwei Kang; Boshi Huang; Zhipeng Huo; Huiqing Liu; Vasanthanathan Poongavanam; Peng Zhan; Xinyong Liu
Journal:  Medchemcomm       Date:  2017-12-01       Impact factor: 3.597

5.  Traceless Staudinger ligation enabled parallel synthesis of proteolysis targeting chimera linker variants.

Authors:  Troy A Bemis; James J La Clair; Michael D Burkart
Journal:  Chem Commun (Camb)       Date:  2021-01-06       Impact factor: 6.222

6.  Reversible Functionalization of Clickable Polyacrylamide Gels with Protein and Graft Copolymers.

Authors:  Hector D Neira; Shaheen Jeeawoody; Amy E Herr
Journal:  Adv Funct Mater       Date:  2020-08-26       Impact factor: 18.808

Review 7.  DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions.

Authors:  Patrick R Fitzgerald; Brian M Paegel
Journal:  Chem Rev       Date:  2020-10-12       Impact factor: 72.087

8.  Thermogravimetric analysis, kinetic study, and pyrolysis-GC/MS analysis of 1,1'-azobis-1,2,3-triazole and 4,4'-azobis-1,2,4-triazole.

Authors:  Chenhui Jia; Yuchuan Li; Shujuan Zhang; Teng Fei; Siping Pang
Journal:  Chem Cent J       Date:  2018-03-01       Impact factor: 4.215

Review 9.  Click-chemistry approaches to π-conjugated polymers for organic electronics applications.

Authors:  Assunta Marrocchi; Antonio Facchetti; Daniela Lanari; Stefano Santoro; Luigi Vaccaro
Journal:  Chem Sci       Date:  2016-06-27       Impact factor: 9.825

10.  Identification of a Potent Phosphoinositide 3-Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs.

Authors:  Tracey Pirali; Elisa Ciraolo; Silvio Aprile; Alberto Massarotti; Alex Berndt; Alessia Griglio; Marta Serafini; Valentina Mercalli; Clarissa Landoni; Carlo Cosimo Campa; Jean Piero Margaria; Rangel L Silva; Giorgio Grosa; Giovanni Sorba; Roger Williams; Emilio Hirsch; Gian Cesare Tron
Journal:  ChemMedChem       Date:  2017-08-31       Impact factor: 3.466

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