Literature DB >> 23485081

Is synthesis the main hurdle for the generation of diversity in compound libraries for screening?

Warren Rjd Galloway1, David R Spring.   

Abstract

BACKGROUND: 'Diversity' is often cited as a crucial consideration when generating compound collections for biological screening. However, what exactly does one mean by 'diversity' and why is it important?
OBJECTIVE: How can diversity be incorporated into compound collections and what are the theoretical and technical challenges this poses? In this editorial, we comment on various factors involved in the creation of structurally, and most crucially, functionally diverse compound libraries.
CONCLUSIONS: In particular, we highlight the central role played by organic synthesis and discuss the value of diversity-driven synthetic approaches in the search for new biologically active molecules with potentially exciting and unusual biological properties.

Year:  2009        PMID: 23485081     DOI: 10.1517/17460440902916606

Source DB:  PubMed          Journal:  Expert Opin Drug Discov        ISSN: 1746-0441            Impact factor:   6.098


  8 in total

1.  Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules.

Authors:  Warren R J D Galloway; Albert Isidro-Llobet; David R Spring
Journal:  Nat Commun       Date:  2010-09-21       Impact factor: 14.919

2.  Diversity-oriented synthesis of macrocyclic peptidomimetics.

Authors:  Albert Isidro-Llobet; Tiffanie Murillo; Paula Bello; Agostino Cilibrizzi; James T Hodgkinson; Warren R J D Galloway; Andreas Bender; Martin Welch; David R Spring
Journal:  Proc Natl Acad Sci U S A       Date:  2011-03-07       Impact factor: 11.205

3.  Late-stage chemoselective functional-group manipulation of bioactive natural products with super-electrophilic silylium ions.

Authors:  Trandon A Bender; Philippa R Payne; Michel R Gagné
Journal:  Nat Chem       Date:  2017-09-18       Impact factor: 24.427

4.  Chemical Space Overlap with Critical Protein-Protein Interface Residues in Commercial and Specialized Small-Molecule Libraries.

Authors:  Yubing Si; David Xu; Khuchtumur Bum-Erdene; Mona K Ghozayel; Baocheng Yang; Paul A Clemons; Samy O Meroueh
Journal:  ChemMedChem       Date:  2018-12-20       Impact factor: 3.466

5.  Limonin as a Starting Point for the Construction of Compounds with High Scaffold Diversity.

Authors:  Lucia Furiassi; Emily J Tonogai; Paul J Hergenrother
Journal:  Angew Chem Int Ed Engl       Date:  2021-06-10       Impact factor: 16.823

6.  Cycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery.

Authors:  Thomas A King; Hannah L Stewart; Kim T Mortensen; Andrew J P North; Hannah F Sore; David R Spring
Journal:  European J Org Chem       Date:  2019-07-29

Review 7.  Macrocyclic drugs and synthetic methodologies toward macrocycles.

Authors:  Xufen Yu; Dianqing Sun
Journal:  Molecules       Date:  2013-05-24       Impact factor: 4.411

8.  iVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancer.

Authors:  Agostino Cilibrizzi; Giuseppe Floresta; Vincenzo Abbate; Maria Paola Giovannoni
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

  8 in total

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