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Fragment-to-Lead Medicinal Chemistry Publications in 2018. | LitMetric

Fragment-to-Lead Medicinal Chemistry Publications in 2018.

J Med Chem

Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, United Kingdom.

Published: May 2020

AI Article Synopsis

Article Abstract

This Perspective, the fourth in an annual series, summarizes fragment-to-lead (F2L) success stories published during 2018. Topics such as target class, screening methods, physicochemical properties, and ligand efficiency are discussed for the 2018 examples as well as for the combined 111 F2L examples covering 2015-2018. While the overall properties of fragments and leads have remained constant, a number of new trends are noted, for example, broadening of target class coverage and application of FBDD to covalent inhibitors. Moreover, several studies make use of fragment hits that were previously described in the literature, illustrating that fragments are versatile starting points that can be optimized to structurally diverse leads. By focusing on success stories, the hope is that this Perspective will identify and inform best practices in fragment-based drug discovery.

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.9b01581DOI Listing

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