Robert W. Hicklin

Abstract 7092: Highly potent and mutant-selective p53 Y220C reactivators with best-in-class potential

Chiou-Hong Lin, Benjamin C. Milgram, Brendon Ladd, Weixue Wang et autres

Abstract Background: The tumor suppressor p53, encoded by the TP53 gene, is a transcription factor that regulates genes involved in DNA repair, cell cycle arrest, senescence, and apoptosis. TP53 is the most frequently altered tumor suppressor gene with mutations occurring in over …

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Discovery of an ITK and TRK kinase inhibitor for the potential topical treatment of atopic dermatitis

Jennifer Lynn Duffen, Kimberly K. Crouse, Lin Ji, Amy L. Brault et autres

Interleukin-2-inducible T cell kinase is expressed by T cells and amplifies T cell receptor-dependent signals. Interleukin-2-inducible T cell kinase deletion or inhibition reduces production of interleukin-4 and interleukin-13, key drivers of atopic dermatitis. Nerve growth factor signals via the receptor tropomyosin-related kinase …

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Peptidylarginine Deiminase (PAD) Inhibitor Optimization through Displacement of a Trapped Water Molecule

Mark E. Schnute, Gary M. Chinigo, Kentaro Futatsugi, Masaya Yamaguchi et autres

Excess protein citrullination, a post-translational modification converting arginine to citrulline, has been associated with a range of autoimmune and neurological disorders, as well as cancers. Protein citrullination is mediated by the peptidylarginine deiminase enzyme family (PAD1–4), and inhibition of one or several …

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Demonstration of a Multikilogram-Scale Birch Reduction and Evaluation of Alternative Synthetic Routes to a Ketalized Cyclohexene Derivative

Adam E. Goetz, Joel T. Arcari, Scott W. Bagley, Robert W. Hicklin et autres

We report the successful manufacture of several >50 kg batches of a key intermediate via a Birch reduction that utilized liquified ammonia as well as lithium metal. With an eye toward continued scalability, we explored two alternative procedures to obtain the same …

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Correction to “Automated Nanomole-Scale Reaction Screening toward Benzoate Bioisosteres: A Photocatalyzed Approach to Highly Elaborated Bicyclo[1.1.1]Pentanes”

James J. Mousseau, Matthew A. Perry, Mark W. Bundesmann, Gary M. Chinigo et autres

ADVERTISEMENT RETURN TO ISSUEPREVCorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to "Automated Nanomole-Scale Reaction Screening toward Benzoate Bioisosteres: A Photocatalyzed Approach to Highly Elaborated Bicyclo[1.1.1]Pentanes"James J. MousseauJames J. MousseauMore by James J. Mousseauhttps://orcid.org/0000-0002-5712-9222, Matthew A. PerryMatthew A. PerryMore by Matthew A. Perry, Mark …

Automated Nanomole-Scale Reaction Screening toward Benzoate Bioisosteres: A Photocatalyzed Approach to Highly Elaborated Bicyclo[1.1.1]Pentanes

James J. Mousseau, Matthew A. Perry, Mark W. Bundesmann, Gary M. Chinigo et autres

Through the application of high-throughput nanoscale optimization, a mild, photocatalyzed, Minisci-like protocol was developed to access highly functionalized 1,3-disubstituted bicyclopentanes. The benzoate-isosteric compounds were prepared using a readily available organic photocatalyst, mitigating the need for precious metals. The strategy described furnished products …

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A robotic platform for flow synthesis of organic compounds informed by AI planning

Connor W. Coley, Dale A. Thomas, Justin A. M. Lummiss, Jonathan N. Jaworski et autres

The synthesis of complex organic molecules requires several stages, from ideation to execution, that require time and effort investment from expert chemists. Here, we report a step toward a paradigm of chemical synthesis that relieves chemists from routine tasks, combining artificial intelligence-driven …

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CCDC 1851845: Experimental Crystal Structure Determination

Evijola Llabani, Robert W. Hicklin, Hyang Yeon Lee, Stephen E. Motika et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

CCDC 1849494: Experimental Crystal Structure Determination

Evijola Llabani, Robert W. Hicklin, Hyang Yeon Lee, Stephen E. Motika et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Diverse compounds from pleuromutilin lead to a thioredoxin inhibitor and inducer of ferroptosis

Evijola Llabani, Robert W. Hicklin, Hyang Yeon Lee, Stephen E. Motika et autres

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Flow Chemistry in Organic Synthesis

Timothy F. Jamison, Guido Koch, Aaron B. Beeler, Rachel L. Beingessner et autres

6 Hazardous Reagents in Continuous-Flow Chemistry

Robert W. Hicklin, Alexandra E. Strom, Evan D. Styduhar, Timothy F. Jamison

Abstract Continuous-flow technology enables the use of hazardous reagents and the safe handling of hazardous intermediates. This chapter focuses on the application of continuous-flow techniques in reactions involving reactive organometallic reagents, hazardous nitrogen- and halogen-based reagents, oxidants, and toxic low-molecular-weight reagents.