Shane W Krska
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Explore the profile of Shane W Krska including associated specialties, affiliations and a list of published articles.
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58
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1151
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Recent Articles
1.
Tyagarajan S, Andrews C, Beshore D, Buevich A, Curran P, Dandliker P, et al.
ACS Med Chem Lett
. 2024 Oct;
15(10):1787-1794.
PMID: 39411537
The science of drug discovery involves multiparameter optimization of molecular structures through iterative design-make-test cycles. For medicinal chemistry library synthesis, traditional workflows involve the isolation of each individual compound, gravimetric...
2.
Golden D, Flynn K, Aikonen S, Hanneman C, Kalyani D, Krska S, et al.
Chem
. 2024 Aug;
10(5):1593-1605.
PMID: 39108591
Site-selective functionalization of the heterobenzylic C(sp)-H bonds of pyridines and related heteroaromatic compounds presents challenges associated with the basic nitrogen atom and the variable reactivity among different positions on the...
3.
Webb E, Cheng K, Winton W, Klein B, Bowden G, Horikawa M, et al.
J Am Chem Soc
. 2024 Apr;
146(15):10581-10590.
PMID: 38580459
Positron emission tomography is a widely used imaging platform for studying physiological processes. Despite the proliferation of modern synthetic methodologies for radiolabeling, the optimization of these reactions still primarily relies...
4.
Chen S, He C, Kong M, Wang J, Lin S, Krska S, et al.
Nat Synth
. 2024 Mar;
2(10):998-1008.
PMID: 38463240
Pharmaceutical and agrochemical discovery efforts rely on robust methods for chemical synthesis that rapidly access diverse molecules. Cross-coupling reactions are the most widely used synthetic methods, but these methods typically...
5.
Wleklinski M, Carpenter P, Dykstra K, Donofrio A, Nowak T, Krska S, et al.
SLAS Technol
. 2024 Feb;
29(2):100126.
PMID: 38423211
High-throughput experimentation (HTE) has become more widely utilized in drug discovery for rapid reaction optimization and generation of large synthetic compound arrays. While this has accelerated medicinal chemistry design, make,...
6.
Chen S, Krska S, Stahl S
Acc Chem Res
. 2023 Dec;
56(24):3604-3615.
PMID: 38051914
ConspectusCross-coupling methods are the most widely used synthetic methods in medicinal chemistry. Existing reactions are dominated by methods such as amide coupling and arylation reactions that form bonds to sp-hybridized...
7.
Maity S, Lopez M, Bates D, Lin S, Krska S, Stahl S
J Am Chem Soc
. 2023 Aug;
145(36):19832-19839.
PMID: 37642292
Site-selective radical reactions of benzylic C-H bonds are now highly effective methods for C(sp-H) functionalization and cross-coupling. The existing methods, however, are often ineffective with heterobenzylic C-H bonds in alkyl-substituted...
8.
Chambers R, Weaver J, Kim J, Hoar J, Krska S, White M
Proc Natl Acad Sci U S A
. 2023 Jul;
120(29):e2300315120.
PMID: 37428920
An emerging trend in small-molecule pharmaceuticals, generally composed of nitrogen heterocycles (-heterocycles), is the incorporation of aliphatic fragments. Derivatization of the aliphatic fragments to improve drug properties or identify metabolites...
9.
Cao W, Maza J, Chernyak N, Flygare J, Krska S, Toste F, et al.
Bioconjug Chem
. 2023 Feb;
34(3):510-517.
PMID: 36787347
Cysteines are routinely used as site-specific handles to synthesize antibody-drug conjugates for targeted immunotherapy applications. Michael additions between thiols and maleimides are some of the most common methods for modifying...
10.
Prieto Kullmer C, Kautzky J, Krska S, Nowak T, Dreher S, MacMillan D
Science
. 2022 Apr;
376(6592):532-539.
PMID: 35482871
Reaction generality is crucial in determining the overall impact and usefulness of synthetic methods. Typical generalization protocols require a priori mechanistic understanding and suffer when applied to complex, less understood...