Expanding the medicinal chemistry synthetic toolbox

Boström, Jonas and Brown, Dean G. and Young, Robert J. and Keserű, György Miklós (2018) Expanding the medicinal chemistry synthetic toolbox. NATURE REVIEWS DRUG DISCOVERY, 17 (10). pp. 709-727. ISSN 1474-1776

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The key objectives of medicinal chemistry are to efficiently design and synthesize bioactive compounds that have the potential to become safe and efficacious drugs. Most medicinal chemistry programmes rely on screening compound collections populated by a range of molecules derived from a set of known and robust chemistry reactions. Analysis of the role of synthetic organic chemistry in subsequent hit and lead optimization efforts suggests that only a few reactions dominate. Thus, the uptake of new synthetic methodologies in drug discovery is limited. Starting from the known limitations of reaction parameters, synthesis design tools, synthetic strategies and innovative chemistries, here we highlight opportunities for the expansion of the medicinal chemists’ synthetic toolbox. More intense crosstalk between synthetic and medicinal chemists in industry and academia should enable enhanced impact of new methodologies in future drug discovery. © 2018 Springer Nature Limited. All rights reserved.

Item Type: Article
Additional Information: Cited By :3 Export Date: 3 January 2019 CODEN: NRDDA Correspondence Address: Keserü, G.M.; Medicinal Chemistry Research Group, Research Center for Natural Sciences, Hungarian Academy of SciencesHungary; email: Funding details: 2017–1.2.1-NKP-2017-00002 Funding details: Nemzeti Kutatási, Fejlesztési és Innovációs Hivatal Funding text 1: G.M.K. is supported by the National Brain Research Program (2017–1.2.1-NKP-2017-00002) of the National Research, Development and Innovation Office, Hungary.
Subjects: R Medicine / orvostudomány > RS Pharmacy and materia medica / gyógyszerészet, gyógyászati eszközök
Depositing User: MTMT SWORD
Date Deposited: 17 Jan 2019 14:15
Last Modified: 17 Jan 2019 14:15

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