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Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

JOURNAL ARTICLE published 23 December 2021 in Journal of Medicinal Chemistry

Research funded by Norges Forskningsr??d (262613,267639) | Academy of Finland (287063,294085,319299) | South-Eastern Norway Regional Health Authority (15/00779-2,16/00528-9,2015012,2019090,2021035)

Authors: Ruben G. G. Leenders | Shoshy Alam Brinch | Sven T. Sowa | Enya Amundsen-Isaksen | Albert Galera-Prat | Sudarshan Murthy | Sjoerd Aertssen | Johannes N. Smits | Piotr Nieczypor | Eddy Damen | Anita Wegert | Marc Nazaré | Lari Lehtiö | Jo Waaler | Stefan Krauss

Discovery of (2S,4R)-1-(2-Aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic Acid Hydrochloride (GAP-134)13, an Orally Active Small Molecule Gap-Junction Modifier for the Treatment of Atrial Fibrillation

JOURNAL ARTICLE published 26 February 2009 in Journal of Medicinal Chemistry

Authors: John A. Butera | Bjarne Due Larsen | James K. Hennan | Edward Kerns | Li Di | Asaf Alimardanov | Robert E. Swillo | Gwen A. Morgan | Kun Liu | Qiang Wang | Eric I. Rossman | Rayomand Unwalla | Leonard McDonald | Christine Huselton | Jørgen S. Petersen

Going beyond Binary: Rapid Identification of Protein–Protein Interaction Modulators Using a Multifragment Kinetic Target-Guided Synthesis Approach

JOURNAL ARTICLE published 13 April 2023 in Journal of Medicinal Chemistry

Research funded by National Institutes of Health (P01CA118210) | The James and Esther King Biomedical Research Program (NIR 07KN-08)

Authors: Katya Nacheva | Sameer S. Kulkarni | Mintesinot Kassu | David Flanigan | Andrii Monastyrskyi | Iredia D. Iyamu | Kenichiro Doi | Megan Barber | Niranjan Namelikonda | Jeremiah D. Tipton | Prakash Parvatkar | Hong-Gang Wang | Roman Manetsch

Dual-Bioorthogonal Catalysis by a Palladium Peptide Complex

JOURNAL ARTICLE published 9 March 2023 in Journal of Medicinal Chemistry

Research funded by Deutsche Forschungsgemeinschaft (EXC 2008 390540038) | Wellcome Trust (203149) | UniSysCat (449713269)

Authors: Ana M. Pérez-López | Adam Belsom | Linus Fiedler | Xiaoyi Xin | Juri Rappsilber

Structure-Based Design, Synthesis, and A-Site rRNA Cocrystal Complexes of Functionally Novel Aminoglycoside Antibiotics:  C2‘ ‘ Ether Analogues of Paromomycin

JOURNAL ARTICLE published 1 May 2007 in Journal of Medicinal Chemistry

Authors: Stephen Hanessian | Janek Szychowski | Susanta Sekhar Adhikari | Guillermo Vasquez | Pachamuthu Kandasamy | Eric E. Swayze | Michael T. Migawa | Ray Ranken | Boris François | Julia Wirmer-Bartoschek | Jiro Kondo | Eric Westhof

Binding and Interaction of Dinitroanilines with Apicomplexan and Kinetoplastid α-Tubulin

JOURNAL ARTICLE published 1 August 2006 in Journal of Medicinal Chemistry

Authors: Arpita Mitra | David Sept

Dual-Mode HDAC Prodrug for Covalent Modification and Subsequent Inhibitor Release

JOURNAL ARTICLE published 11 June 2015 in Journal of Medicinal Chemistry

Research funded by National Institute of General Medical Sciences (R01 GM098435,R01 GM101467,R01 GM40602)

Authors: Kevin B. Daniel | Eric D. Sullivan | Yao Chen | Joshua C. Chan | Patricia A. Jennings | Carol A. Fierke | Seth M. Cohen

Synthesis and Cytotoxic Evaluation of Combretafurans, Potential Scaffolds for Dual-Action Antitumoral Agents

JOURNAL ARTICLE published 1 August 2006 in Journal of Medicinal Chemistry

Authors: Tracey Pirali | Sara Busacca | Lorena Beltrami | Daniela Imovilli | Francesca Pagliai | Gianluca Miglio | Alberto Massarotti | Luisella Verotta | Gian Cesare Tron | Giovanni Sorba | Armando A. Genazzani

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode

JOURNAL ARTICLE published 23 February 2017 in Journal of Medicinal Chemistry

Authors: Elizabeth A. Jurica | Ximao Wu | Kristin N. Williams | Andres S. Hernandez | David S. Nirschl | Richard A. Rampulla | Arvind Mathur | Min Zhou | Gary Cao | Chunshan Xie | Biji Jacob | Hong Cai | Tao Wang | Brian J. Murphy | Heng Liu | Carrie Xu | Lori K. Kunselman | Michael B. Hicks | Qin Sun | Dora M. Schnur | Doree F. Sitkoff | Elizabeth A. Dierks | Atsu Apedo | Douglas B. Moore | Kimberly A. Foster | Mary Ellen Cvijic | Reshma Panemangalore | Neil A. Flynn | Brad D. Maxwell | Yang Hong | Yuan Tian | Jason J. Wilkes | Bradley A. Zinker | Jean M. Whaley | Joel C. Barrish | Jeffrey A. Robl | William R. Ewing | Bruce A. Ellsworth

Synthesis and Characterization of a Novel Gadolinium-Based Contrast Agent for Magnetic Resonance Imaging of Myelination

JOURNAL ARTICLE published 28 February 2013 in Journal of Medicinal Chemistry

Authors: Luca Frullano | Junqing Zhu | Robert H. Miller | Yanming Wang

Nitric Oxide Synthase Inhibitors That Interact with Both Heme Propionate and Tetrahydrobiopterin Show High Isoform Selectivity

JOURNAL ARTICLE published 22 May 2014 in Journal of Medicinal Chemistry

Research funded by National Institutes of Health (GM049725)

Authors: Soosung Kang | Wei Tang | Huiying Li | Georges Chreifi | Pavel Martásek | Linda J. Roman | Thomas L. Poulos | Richard B. Silverman

7-Deazaadenines Bearing Polar Substituents:  Structure−Activity Relationships of New A1 and A3 Adenosine Receptor Antagonists

JOURNAL ARTICLE published 1 November 2000 in Journal of Medicinal Chemistry

Authors: Sonja Hess | Christa E. Müller | Wolfram Frobenius | Ulrike Reith | Karl-Norbert Klotz | Kurt Eger

Application of the λ-Dynamics Method To Evaluate the Relative Binding Free Energies of Inhibitors to HCV Protease

JOURNAL ARTICLE published 1 December 2003 in Journal of Medicinal Chemistry

Authors: Zhuyan Guo | James Durkin | Thierry Fischmann | Richard Ingram | Andrew Prongay | Rumin Zhang | Vincent Madison

Design and Synthesis of Phosphotyrosine Peptidomimetic Prodrugs

JOURNAL ARTICLE published 1 June 2006 in Journal of Medicinal Chemistry

Authors: Hugo Garrido-Hernandez | Kyung D. Moon | Robert L. Geahlen | Richard F. Borch

Targeting Peroxisome Proliferator-Activated Receptor Delta (PPARδ): A Medicinal Chemistry Perspective

JOURNAL ARTICLE published 24 September 2020 in Journal of Medicinal Chemistry

Research funded by National Research Foundation of Korea (NRF-2017M3A9G7073088,NRF-2017R1C1B1005599,NRF-2018R1D1A1B07047143,NRF-2020R1C1C1007221,NRF-2020R1C1C1009350)

Authors: Tara Man Kadayat | Aarajana Shrestha | Yong Hyun Jeon | Hongchan An | Jina Kim | Sung Jin Cho | Jungwook Chin

1-[(ω-Aminoalkyl)amino]-4-[N-(ω-aminoalkyl)carbamoyl]-9-oxo-9,10-dihydro- acridines as Intercalating Cytotoxic Agents:  Synthesis, DNA Binding, and Biological Evaluation

JOURNAL ARTICLE published 1 November 1997 in Journal of Medicinal Chemistry

Authors: Ippolito Antonini | Paolo Polucci | Terence C. Jenkins | Lloyd R. Kelland | Ernesto Menta | Nicoletta Pescalli | Barbara Stefanska | Jan Mazerski | Sante Martelli

Fluorine-Substituted Cyclofenil Derivatives as Estrogen Receptor Ligands:  Synthesis and Structure−Affinity Relationship Study of Potential Positron Emission Tomography Agents for Imaging Estrogen Receptors in Breast Cancer

JOURNAL ARTICLE published 1 April 2006 in Journal of Medicinal Chemistry

Authors: Jai Woong Seo | John S. Comninos | Dae Yoon Chi | Dong Wook Kim | Kathryn E. Carlson | John A. Katzenellenbogen

Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α2α

JOURNAL ARTICLE published 1 March 2007 in Journal of Medicinal Chemistry

Authors: Katherine L. Lee | Megan A. Foley | Lihren Chen | Mark L. Behnke | Frank E. Lovering | Steven J. Kirincich | Weiheng Wang | Jaechul Shim | Steve Tam | Marina W. H. Shen | SooPeang Khor | Xin Xu | Debra G. Goodwin | Manjunath K. Ramarao | Cheryl Nickerson-Nutter | Frances Donahue | M. Sherry Ku | James D. Clark | John C. McKew

Synthesis and Antiviral Activity of Novel 5-(1-Cyanamido-2-haloethyl) and 5-(1-Hydroxy(or methoxy)-2-azidoethyl) Analogues of Uracil Nucleosides

JOURNAL ARTICLE published 1 October 2001 in Journal of Medicinal Chemistry

Authors: Rakesh Kumar | Dinesh Rai | Sanjay K. Sharma | Holly A. Saffran | Ryan Blush | D. Lorne J. Tyrrell

Synthesis and Biological Evaluation of Selective Aromatase Expression Regulators in Breast Cancer Cells

JOURNAL ARTICLE published 1 April 2007 in Journal of Medicinal Chemistry

Authors: Bin Su | Serena Landini | Danyetta D. Davis | Robert W. Brueggemeier