Výsledky vyhledávání - "Kevin D. Hesp"

Preparation and Functionalization of Mono- and Polyfluoroepoxides via Fluoroalkylation of Carbonyl Electrophiles

Autor: Shuo Guo, Wei Sun, Joseph W. Tucker, Kevin D. Hesp, Nathaniel K. Szymczak

Publikováno v: Chemistry (Weinheim an der Bergstrasse, Germany).

We outline a new synthetic method to prepare mono- and polyfluoroepoxides from a diverse pool of electrophiles (ketones, acyl chlorides, esters) and fluoroalkyl anion equivalents. The initially formed α-fluoro alkoxides undergo subsequent intramolec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05ef2c3287fc9fbc3a1864718ed81189
https://pubmed.ncbi.nlm.nih.gov/36478306

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Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel β-Arrestin Antagonist Activity

Autor: Jessica Ward, John Litchfield, Keith Riccardi, Carina Tan, Elnaz Menhaji-Klotz, Markus Boehm, Paula M. Loria, Kevin D. Hesp, Janice A. Brown

Publikováno v: ACS Med Chem Lett

[Image: see text] The atypical chemokine receptor CXCR7 has been studied in various disease settings including immunological diseases and heart disease. Efforts to elucidate the role of CXCR7 have been limited by the lack of suitable chemical tools w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1e6eb2ef408c6d5c336c25957638d3f
https://doi.org/10.1021/acsmedchemlett.0c00163

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Mechanistic study of enantioselective Pd-catalyzed C(sp(3))–H activation of thioethers involving two distinct stereomodels

Autor: Daniel C. Schmitt, Paul F. Richardson, Tyler G. Saint-Denis, Jason S. Chen, Yajing Lian, Kevin D. Hesp, Nelson Y. S. Lam, Nikita Chekshin, Jin-Quan Yu, Chan Woo Huh, Jeff Elleraas

Publikováno v: ACS Catal

Enantioselective C(sp(3))–H activation has gained considerable attention from the synthetic chemistry community. Despite the intense interest in these reactions, the mechanisms responsible for enantioselection are still vague. In the course of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3289d8d5c73f1ac6d9aa498e6a1e083a
https://europepmc.org/articles/PMC9098185/

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Discovery and evaluation of non-basic small molecule modulators of the atypical chemokine receptor CXCR7

Autor: Chris Limberakis, Allyn T. Londregan, Steven B. Coffey, Gary Erik Aspnes, Janice A. Brown, Kevin D. Hesp, Rhys M. Jones, Elnaz Menhaji-Klotz, Esther C.Y. Lee, Markus Boehm

Publikováno v: Bioorganicmedicinal chemistry letters. 50

The atypical chemokine receptor C-X-C chemokine receptor type 7 (CXCR7) is an attractive therapeutic target for a variety of cardiac and immunological diseases. As a strategy to mitigate known risks associated with the development of higher molecular

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::814f75791497d041702db0bd1f7ff5db
https://pubmed.ncbi.nlm.nih.gov/34400299

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Late-stage synthesis and application of photoreactive probes derived from direct benzoylation of heteroaromatic C-H bonds

Autor: Jun Xiao, Graham M. West, Kevin D. Hesp

Publikováno v: Organicbiomolecular chemistry. 18(19)

A C–H functionalization strategy for the expedient access to photoreactive chemical probes of commonly found heterocyclic fragments or drug molecules of pharmaceutical relevance is described. A series of aryl glyoxylic acid reagents featuring penda

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d909465637d99e88d28bf7f49f0bc6c0
https://pubmed.ncbi.nlm.nih.gov/32373883

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Asymmetric Synthesis of a Potent CXCR7 Modulator Featuring a Hindered Tertiary β-Amino Amide Stereocenter

Autor: François Godin, Daniel P. Canterbury, Samuel Desjardins, Malken Bayrakdarian, David Austen Perry, Jeffrey S. Albert, Kevin D. Hesp

Publikováno v: Organic Letters. 20:5336-5339

A practical and asymmetric synthesis of a small-molecule CXCR7 modulator featuring a highly functionalized and hindered tertiary β-amino amide framework is reported. The cornerstone of this strategy relied on the intermediacy of a reactive aziridini

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3aea7c2b43df0533c2d7c956b98592f6
https://doi.org/10.1021/acs.orglett.8b02261

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Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents

Publikováno v: Journal of Medicinal Chemistry. 61:5704-5718

The optimization of a new class of small molecule PCSK9 mRNA translation inhibitors is described. The potency, physicochemical properties, and off-target pharmacology associated with the hit compound (1) were improved by changes to two regions of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46075104e513dd56e96e55dc41b689b9
https://doi.org/10.1021/acs.jmedchem.8b00650

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Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing

Publikováno v: Journal of the American Chemical Society, vol 140, iss 21
Rouet, Romain; Thuma, Benjamin A; Roy, Marc D; Lintner, Nathanael G; Rubitski, David M; Finley, James E; et al.(2018). Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing.. Journal of the American Chemical Society, 140(21), 6596-6603. doi: 10.1021/jacs.8b01551. UC Berkeley: Retrieved from: http://www.escholarship.org/uc/item/61k3t664

CRISPR-Cas RNA-guided endonucleases hold great promise for disrupting or correcting genomic sequences through site-specific DNA cleavage and repair. However, the lack of methods for cell- and tissue-selective delivery currently limits both research a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9af967c5dc058dcd0e0a6cfe05eb8b81
https://doi.org/10.1021/jacs.8b01551

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