Privileged Scaffolds for Library Design and Drug Discovery
TLDR
This review explores the concept of using privileged scaffolds to identify biologically active compounds through building chemical libraries by revealing through four selected examples the present state of the art in privileged scaffold library synthesis.About:
This article is published in Current Opinion in Chemical Biology.The article was published on 2010-06-01 and is currently open access. It has received 1160 citations till now.read more
Citations
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Click Chemistry for Drug Development and Diverse Chemical–Biology Applications
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Pharmacological inhibition of cystine–glutamate exchange induces endoplasmic reticulum stress and ferroptosis
Scott J. Dixon,Darpan N Patel,Matthew Welsch,Rachid Skouta,Eric D Lee,Miki Hayano,Ajit G. Thomas,Caroline E Gleason,Nicholas P. Tatonetti,Barbara S. Slusher,Brent R. Stockwell +10 more
TL;DR: Dixon, Patel, et al. as mentioned in this paper found that erastin is a very effective inhibitor of system xc− function and that it is over 1000 times more potent than the previously known best inhibitor, sulfasalazine.
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Single-electron transmetalation in organoboron cross-coupling by photoredox/nickel dual catalysis
TL;DR: A mechanistically distinct single-electron transfer-based strategy for the activation of organoboron reagents toward transmetalation that exhibits complementary reactivity patterns.
Journal ArticleDOI
Chalcone: A Privileged Structure in Medicinal Chemistry.
TL;DR: This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry and is expected to be a comprehensive, authoritative, and critical review of the chal cone template to the chemistry community.
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Deep reinforcement learning for de novo drug design
TL;DR: The ReLeaSE method is used to design chemical libraries with a bias toward structural complexity or toward compounds with maximal, minimal, or specific range of physical properties, such as melting point or hydrophobicity.
References
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The evolving role of natural products in drug discovery
Frank E. Koehn,Guy T. Carter +1 more
TL;DR: Recent technological advances that help to address issues such as the lack of compatibility of traditional natural-product extract libraries with high-throughput screening and unrealized expectations from current lead-generation strategies have led to a renewed interest in natural products in drug discovery.
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Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists
Ben E. Evans,Kenneth E. Rittle,Mark G. Bock,Robert M. DiPardo,Roger M. Freidinger,W. L. Whitter,George F. Lundell,Daniel F. Veber,Paul S. Anderson,Raymond S.L. Chang,Victor J. Lotti,D. J. Cerino,Tsing-Bau Chen,Paul J. Kling,K. A. Kunkel,James P. Springer,J. Hirshfield +16 more
TL;DR: 3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
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A Planning Strategy for Diversity‐Oriented Synthesis
TL;DR: Although the distinct goals of DOS do not permit the application of retrosynthetic concepts and thinking, these foundations are being built on, by using parallel logic, to develop a complementary procedure known as forward-Synthetic analysis, which facilitates synthetic planning, communication, and teaching in this evolving discipline.