Rapid Elaboration of Fragments into Leads Applied to Bromodomain-3 Extra-Terminal Domain-Reference-Cited by-同舟云学术

Rapid Elaboration of Fragments into Leads Applied to Bromodomain-3 Extra-Terminal Domain

Published:2023-04-18 Issue:8 Volume:66 Page:5859-5872
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Adams Luke A.¹^ORCID,Wilkinson-White Lorna E.²,Gunzburg Menachem J.¹,Headey Stephen J.¹,Mohanty Biswaranjan²,Scanlon Martin J.¹^ORCID,Capuano Ben¹^ORCID,Mackay Joel P.³,Doak Bradley C.¹

Affiliation:

1. Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville 3052, VIC, Australia

2. Sydney Analytical Core Research Facility, University of Sydney, Camperdown, NSW 2006, Australia

3. School of Life and Environmental Sciences, University of Sydney, Camperdown 2006, NSW, Australia

Funder

National Health and Medical Research Council

Monash Technology Research Platforms

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.3c00137

Reference38 articles.

1. Rapid optimisation of fragments and hits to lead compounds from screening of crude reaction mixtures

2. Rapid Elaboration of Fragments into Leads by X-ray Crystallographic Screening of Parallel Chemical Libraries (REFiLX)

3. Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

4. Efficient discovery of bioactive scaffolds by activity-directed synthesis

5. Marrying chemistry with biology by combining on-chip solution-based combinatorial synthesis and cellular screening

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