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Front Cover: Helenalin Analogues Targeting NF‐κB p65: Thiol Reactivity and Cellular Potency Studies of Varied Electrophiles (ChemMedChem 4/2018)
Author(s) -
Widen John C.,
Kempema Aaron M.,
Baur Jordan W.,
Skopec Hannah M.,
Edwards Jacob T.,
Brown Tenley J.,
Brown Dennis A.,
Meece Frederick A.,
Harki Daniel A.
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800079
Subject(s) - electrophile , chemistry , potency , reactivity (psychology) , front cover , thiol , stereochemistry , methylene , combinatorial chemistry , medicinal chemistry , organic chemistry , biochemistry , in vitro , cover (algebra) , medicine , mechanical engineering , alternative medicine , pathology , engineering , catalysis
The Front Cover shows two race cars, representing an endocyclic enone and an exocyclic methylene butyrolactone, racing to complete hetero‐Michael additions to a biological thiol. This work describes the synthesis of simplified helenalin analogues containing combinations of endocyclic enones and exocyclic methylene butyrolactones. Thiol reactivity kinetics and NF‐κB inhibitory activities of the simplified helenalin analogues is reported, which provides insights into the contributions of the individual electrophiles to biological potency. More information can be found in the Full Paper by Daniel A. Harki et al. on page 303 in Issue 4, 2018 (DOI: 10.1002/cmdc.201700752).