Applications of fluorine in medicinal chemistry
EP Gillis, KJ Eastman, MD Hill… - Journal of medicinal …, 2015 - ACS Publications
The role of fluorine in drug design and development is expanding rapidly as we learn more
about the unique properties associated with this unusual element and how to deploy it with …
about the unique properties associated with this unusual element and how to deploy it with …
Scalable Total Syntheses of N-Linked Tryptamine Dimers by Direct Indole−Aniline Coupling: Psychotrimine and Kapakahines B and F
T Newhouse, CA Lewis, KJ Eastman… - Journal of the American …, 2010 - ACS Publications
This report details the invention of a method to enable syntheses of psychotrimine (1) and
the kapakahines F and B (2, 3) on a gram scale and in a minimum number of steps. …
the kapakahines F and B (2, 3) on a gram scale and in a minimum number of steps. …
Studies on the Mechanism of Action of Prekinamycin, a Member of the Diazoparaquinone Family of Natural Products: Evidence for Both sp2 Radical and …
KS Feldman, KJ Eastman - Journal of the American Chemical …, 2006 - ACS Publications
The putative reductive activation chemistry of the diazoparaquinone antibiotics was modeled
with Bu 3 Sn−H and prekinamycin dimethyl ether along with prekinamycin itself. Reaction …
with Bu 3 Sn−H and prekinamycin dimethyl ether along with prekinamycin itself. Reaction …
Diazonamide synthesis studies: use of Negishi coupling to fashion diazonamide-related biaryls with defined axial chirality
KS Feldman, KJ Eastman, G Lessene - Organic Letters, 2002 - ACS Publications
The syntheses of a bis indole and an indole salicylate with the required axial chirality for
diazonamide A are reported. Atropselectivity in these biaryl systems is enforced by an sp3 …
diazonamide A are reported. Atropselectivity in these biaryl systems is enforced by an sp3 …
An oral androgen receptor RIPTAC for prostate cancer.
K Raina, KJ Eastman, X Yu, CD Forbes, KM Jones… - 2023 - ascopubs.org
184 Background: Resistance to Androgen Receptor Signaling Inhibitors (ARSIs) in prostate
cancer occurs in almost all patients and is driven primarily by genomic alterations in AR and …
cancer occurs in almost all patients and is driven primarily by genomic alterations in AR and …
[HTML][HTML] Regulated induced proximity targeting chimeras (RIPTACs): a novel heterobifunctional small molecule therapeutic strategy for killing cancer cells selectively
…, CD Forbes, R Stronk, JP Rappi Jr, KJ Eastman… - bioRxiv, 2023 - ncbi.nlm.nih.gov
While specific cell signaling pathway inhibitors have yielded great success in oncology,
directly triggering cancer cell death is one of the great drug discovery challenges facing …
directly triggering cancer cell death is one of the great drug discovery challenges facing …
Tactical applications of fluorine in drug design and development
NA Meanwell, KJ Eastman, EP Gillis - Fluorine in Heterocyclic Chemistry …, 2014 - Springer
The increasing utilization of fluorine in drug design parallels advances in understanding the
physicochemical attributes of this element and an enhanced appreciation of how these …
physicochemical attributes of this element and an enhanced appreciation of how these …
A proposal for the mechanism-of-action of diazoparaquinone natural products
KS Feldman, KJ Eastman - Journal of the American Chemical …, 2005 - ACS Publications
Treatment of the representative diazoparaquinone prekinamycin dimethyl ether with Bu 3
SnH/AIBN in aromatic solvents furnishes moderate-to-good yields of formal aryl adducts …
SnH/AIBN in aromatic solvents furnishes moderate-to-good yields of formal aryl adducts …
Bioactivation of cyclopropyl rings by P450: an observation encountered during the optimisation of a series of hepatitis C virus NS5B inhibitors
…, J Zhu, XS Huang, KE Parcella, KJ Eastman… - Xenobiotica, 2018 - Taylor & Francis
Due to its unique C–C and C–H bonding properties, conformational preferences and relative
hydrophilicity, the cyclopropyl ring has been used as a synthetic building block in drug …
hydrophilicity, the cyclopropyl ring has been used as a synthetic building block in drug …
The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase
KJ Eastman, K Parcella, KS Yeung, KA Grant-Young… - …, 2017 - pubs.rsc.org
The development of a series of novel 7-azabenzofurans exhibiting pan-genotype inhibition
of HCV NS5B polymerase via binding to the primer grip site is presented. Many challenges, …
of HCV NS5B polymerase via binding to the primer grip site is presented. Many challenges, …