Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents

Humphries, Paul S.; Bersot, Ross; Kincaid, John; Mabery, Eric; McCluskie, Kerryn; Park, Timothy; Renner, Travis; Riegler, Erin; Steinfeld, Tod; Turtle, Eric D; Wei, Zhi-Liang; Willis, Erik

doi:10.1016/j.bmcl.2017.12.051

Cited by 41 publications

(30 citation statements)

References 29 publications

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“…This compound, KL001, inhibits proteasomal degradation of CRY, lengthens circadian period in a variety of cells and tissues, and blocks glucagon-dependent induction of gluconeogenesis in cultured hepatocytes ( 22 ). Consistent with these observations, a bioavailable derivative of KL001 exhibits antihyperglycemic activity in db/db diabetic mice ( 23 ). Moreover, small-molecule agonists of REV-ERB and ROR improve energy homeostasis ( 24 , 25 ), and REV-ERB agonists impair cancer growth to improve survival in a mouse model of glioblastoma ( 26 ).…”

Section: Introductionmentioning

confidence: 62%

Cell-based screen identifies a new potent and highly selective CK2 inhibitor for modulation of circadian rhythms and cancer cell growth

et al. 2019

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Section: Introductionmentioning

confidence: 62%

Cell-based screen identifies a new potent and highly selective CK2 inhibitor for modulation of circadian rhythms and cancer cell growth

et al. 2019

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“…As a result, energy expenditure increases, adiposity decreases and hepatic steatosis decreases 235 . Finally, in preliminary reports, two different CRY stabilizers were shown to improve glucose tolerance in diet-induced obese mice 236 and db/db mice 237 . The exact mechanism responsible for these metabolic benefits, however, remains to be elucidated.…”

Section: Circadian Moleculesmentioning

confidence: 96%

Circadian clocks and insulin resistance

et al. 2018

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“…27 The conventional approach to cyclic ureas involves carbonylation of variously substituted diamines with phosgene. 28,29 Much effort has been made to replace phosgene by its less toxic analogues, such as dialkyl carbonates, 30,31 triphosgene, [32][33][34] 1,1′-carbonyldiimidazole, 35,36 urea, 37 and others. Novel approaches to these compounds, such as the direct carbonylation with carbon monoxide 38,39 or [3+2] cycloaddition of isocyanoacetates with nitrones, 40 are still emerging, indicating a growing area of interest.…”

Section: Published As Part Of the Special Topic Recent Advances In Ammentioning

confidence: 99%

Nucleophilic Cyclization/Electrophilic Substitution of (2,2-Dialkoxyethyl)ureas: Highly Regioselective Access to Novel 4-(Het)arylimidazolidinones and Benzo[d][1,3]diazepinones

et al. 2020

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Imidazolidin-2-one and 1,3-benzodiazepin-2-one scaffolds are structural motifs of many biologically active compounds. Herein, we report a highly regioselective acid-catalyzed intramolecular nucleophilic cyclization/intermolecular electrophilic substitution reaction sequence of (2,2-dialkoxyethyl)ureas. The reaction benefits from readily available starting materials, a simple workup procedure, moderate to high yields of target compounds, and provides a convenient entry to previously unknown 4-(het)arylimidazolidinones and 5-(het)arylbenzodiazepinones. The proposed mechanism of the reaction is also discussed.

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Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents

Cited by 41 publications

References 29 publications

Cell-based screen identifies a new potent and highly selective CK2 inhibitor for modulation of circadian rhythms and cancer cell growth

Cell-based screen identifies a new potent and highly selective CK2 inhibitor for modulation of circadian rhythms and cancer cell growth

Circadian clocks and insulin resistance

Nucleophilic Cyclization/Electrophilic Substitution of (2,2-Dialkoxyethyl)ureas: Highly Regioselective Access to Novel 4-(Het)arylimidazolidinones and Benzo[d][1,3]diazepinones

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